Kuliah Hipertensi & Glikosida Jantung

PROGRAM STUDI FARMASI
FAKULTAS ILMU KESEHATAN

UNIVERSITAS MUHAMMADIYAH MALANG
Mata Kuliah Farmakologi I

Obat-Obat Anti Hipertensi & Obat
Kardiovaskular
Nikmatul Ikhrom Eka Jayani, S.Farm., M.FarmKlin., Apt.


PUSTAKA
Goodman & Gilmans Manual of
Pharmacology and Therapeutics,
Basic & Clinical Pharmacology
Katzung, Basic & Clinical
Pharmacology 10th ed
Lippincott, Illustrated Reviews
Pharmacology 4th ed
Neal, At a Glance Farmakologi
Medis
Lullman, Colour Atlas of
Pharmacology
dll

Definisi
Hipertensi didefinisikan sebagai salah satu Systolic Blood
Pressure (SBP) > 140 mm Hg atau Diastolic Blood
Pressure (DBP) > 90 mm Hg.

Klasifikasi Tekanan Darah

BP Classification
SBP mHg
DBP mmHg
Normal
<120
and
<80
Prehypertension
120139
or
8089
Stage 1
Hypertension
140159
or
9099
Stage 2
Hypertension
>160
or
>100

Faktor Utama yang mempengaruhi

Tekanan Darah

Pathophisiology of hypertension

Pathophisiology of hypertension

Pathogenesis of hypertension

Kontrol Tubuh terhadap Tekanan Darah

OBAT-OBAT HIPERTENSI
A ACE-1 / ARB / 1-BLOCKER
B BETA-BLOCKER
C Ca-ANTAGONIS, centralling
agent
D DIURETIC
E Etc (lainnya) ex :
reserpine



Mekanisme untuk Kontrol

Tekanan Darah
1= vasodilators,
4= AT II blocker
6= ACE inhibitors
2= -blockers
3=-blockers
5= Centrally sympatholytics
7= diuretics

Antihipertensi Renin Inhibitor,

Angiotensin Converting Enzym Inhibitor (ACE i),
Angiotensin Receptor Blocker (ARB)
Aliskiren
Captopril, Lisinopril,
enalapril
Valsartan, Candesartan,
Telmisartan

Antihipertensi ACE i (1)

Antihipertensi ACE i (2)

1 blockers
The availability of drugs that selectively block 1 adrenergic
receptors without affecting 2 adrenergic receptors is :
Prazosin, terazosin, and doxazosin
Pharmacological Effects.
Initially reduce arteriolar resistance and increase venous
capacitance
During long-term therapy vasodilation persists, but cardiac
output, heart rate, and plasma renin activity return to normal.
Renal blood flow is unchanged during therapy
1 adrenergic blockers cause a variable amount of postural
hypotension, depending on the plasma volume.
first-dose phenomenon, in which symptomatic orthostatic
hypotension occurs within 90 minutes of the initial dose of the
drug or after a dosage increase (50% of patients, especially in
patients who are already receiving a diuretic or an a receptor
antagonist.)

Centralling agent
A. Clonidine
This 2-agonist diminishes central adrenergic outflow, is used
primarily for the treatment of hypertension that has not
responded adequately to treatment with two or more drugs.
Clonidine does not decrease renal blood flow or glomerular
filtration and, therefore, is useful in the treatment of hypertension
complicated by renal disease.
B. Methyldopa
This 2-agonist is converted to methylnorepinephrine centrally
to diminish the adrenergic outflow from the CNS.
This leads to reduced total peripheral resistance and a
decreased blood pressure. Cardiac output is not decreased, and
blood flow to vital organs is not diminished.
It has been used in hypertensive pregnant patients.

Antihipertensi Beta Blocker (1)


Antihipertensi Beta Blocker (2)

Calcium-channel blockers
The calcium-channel blockers are divided into three chemical
classes, each with different pharmacokinetic :
1) Diphenylalkylamines: Verapamil. Verapamil is the least
selective of any calcium-channel blocker and has significant
effects on both cardiac and vascular smooth muscle cells
2) Benzothiazepines: Diltiazem. Like verapamil, diltiazem
affects both cardiac and vascular smooth muscle cells;
however, it has a less pronounced negative inotropic effect on
the heart compared to that of verapamil.
3) Dihydropyridines:
first-generation : Nifedipine
second-generation : Amlodipine, Felodipine, Isradipine,
Nicardipine, and Nisoldipine.
All dihydropyridines have a much greater affinity for vascular
calcium channels than for calcium channels in the heart. They
are therefore particularly attractive in treating hypertension.

Antihipertensi Diuretik
Acetazolamide
Methazolamide
Manitol
Thiazid
Furosemide
Asam Etakrinat
Bumetanid
Amilorid
Triamteren
Spironolakton
reserpine
Reserpine binds tightly to adrenergic storage
vesicles in central and peripheral adrenergic
neurons and remains bound for prolonged periods
of time. The interaction inhibits the vesicular
catecholamine transporter that facilitates vesicular
storage. Thus, nerve endings lose their capacity to
concentrate and store norepinephrine and
dopamine.
Both with reserpine. cardiac output and peripheral
vascular resistance are reduced during long-term
therapy.
Orthostatic hypotension


Obat-Obat Gagal Jantung


Obat Inotropik
Positive inotropic agents enhance cardiac
muscle contractility and thus, increase
cardiac output
inotropic action is the result of an increased
cytoplasmic calcium concentration that
enhances the contractility of cardiac
muscle

A. Digitalis
The cardiac glycosides are often called
digitalis or digitalis glycosides, because most
of the drugs come from the digitalis (foxglove)
plant.
The cardiac glycosides influence the sodium
and calcium ion flows in the cardiac muscle,
thereby increasing contraction of the atrial
and ventricular myocardium (positive
inotropic action).
The drugs have a low therapeutic index.
The most widely used agent is digoxin


Digitalis toxicity is one of the

most commonly encountered
adverse drug reactions
Side effects often can be
managed by discontinuing
cardiac glycoside therapy,
determining serum potassium
levels (decreased K+ enhances
potential for cardiotoxicity), and
if indicated, giving potassium
supplements.

Intoxication signs
(1) cardiac arrhythmias, which under certain
circumstances are life-threatening, e.g., sinus
bradycardia, AV-block, ventricular extrasystoles,
ventricular fibrillation (ECG);
(2) CNS disturbances altered color vision
(xanthopsia), agitation, confusion, nightmares,
hallucinations
(3) gastrointestinal anorexia, nausea, vomiting,
diarrhea;
(4) renal loss of electrolytes and water, which must be
differentiated from mobilization of accumulated
edema fluid that occurs with therapeutic dosage

B. -Adrenergic agonists
-Adrenergic stimulation improves cardiac
performance by causing positive inotropic
effects and vasodilation.
Dopamine and Dobutamine is the most
commonly used
C. Phosphodiesterase inhibitors
Amrinone and milrinone are
phosphodiesterase inhibitors

36

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PROGRAM STUDI FARMASI

FAKULTAS ILMU KESEHATAN

Mata Kuliah Farmakologi I

Nikmatul Ikhrom Eka Jayani, S.Farm., M.FarmKlin., Apt.

PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

Klasifikasi Tekanan Darah

PROGRAM STUDI FARMASI

Faktor Utama yang mempengaruhi

PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

Kontrol Tubuh terhadap Tekanan Darah

PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

Mekanisme untuk Kontrol

PROGRAM STUDI FARMASI

Antihipertensi Renin Inhibitor,

PROGRAM STUDI FARMASI

Antihipertensi ACE i (1)

PROGRAM STUDI FARMASI

Antihipertensi ACE i (2)

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PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

Antihipertensi Beta Blocker (1)

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Antihipertensi Beta Blocker (2)

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PROGRAM STUDI FARMASI

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Obat-Obat Gagal Jantung

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PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

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Digitalis toxicity is one of the

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PROGRAM STUDI FARMASI

PROGRAM STUDI FARMASI

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