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Hyperthensive
Drugs
Dr. Yogi P. R.
Medical Faculty
Swadaya Gunung Jati University
Cirebon 2009
Pathophysiology
= X
Contributions to BP = combination of
genetic inheritance, psychological stress,
and dietary factors
Abnormalities in the ANS, baroreceptor
reflexes, the renin-angiotensin-
aldosterone system and the kidney (all
used in regulating BP).
Hypertension
(artery stenosis)
susceptive
Hormonal defects
(obesity, stress, salt intake, lack of
(Cushings syndrome,
Mg2+, K+, Ca2+, ethanol dose,
phaeochromocytoma)
smoking)
Mechanical defect
(coarctation of aorta)
non-susceptive Hypertension in pregnancy
(positive family history, insulin Drug-induced hypertension
resistance, age, sex, defect of (sympatomimetics,
local vasomotoric regualtion) glucocorticoids)
Neurologic desease
Classification
JNC-VII
JNC VI
Stages of Hypertension
Stage Diastolic Range (mm Systolic Range (mm
Hg) Hg)
A. Non-pharmacological - lifestyle
THIAZIDES
hydrochlorothiazide, clopamid, chlorthalidone
indapamid, metipamid
Mechanism of action:
- Menghambat transport Na+, K+ dan Cl-
- of Ca2+ and Mg2+ excretion
- Memiliki efek vasodilatasi pembuluh darah pulmo (unknown
mechanism)
Adverse Effect :
- hypokalemic metabolic alkalosis (increased
excretion of K+)
- ototoxicity (dose dependent, reversible)
- decrease of Mg2+ plasma concentration
(hypomagnesemia)
- hyperuricemia
- risk of dehydration (> 4 L urine/ 24 h)
DIURETICS HEMAT KALIUM
Spironolacton
- Diuretik lemah
- Digunakan dgn diuretik lain utk mencegah
atau mengurangi hipokalemia dr diuretik lain
Mechanism of action:
- Antagonis spesifik dari aldosteron pilihan
utama utk hiperaldosteronisme primer
Adverse Effect :
Ginekomastia
Mastodinia
Menstruasi tidak teratur
Berkurangnya libido pd pria
2. Drugs influencing sympathetic nerves
a) -adrenoreceptor antagonists
Mechanism of action:
- Vasodilatasi dan menurunkan BP dgn menghambat noradrenalin
pd 1 receptors (vascular smooth muscle)
competitive with:
a. short-term action:
non-selective - phentolamine
selective - prazosin, uradipil,
b. long-acting
antagonists - doxazosin, terazosin
b) -adrenoreceptor antagonists
Mechanism of action:
1. Mengurangi denyut jantung dan kontraktilitas myocard CO
berkurang
2. Menghambat pelepasan NE melalui hambatan reseptor 2
prasinaps
3. Menghambat sekresi renin melalui hambatan 1 di ginjal
4. Efek sentral
-adrenoreceptor antagonists
cardio-selective:
blockers atenolol, metoprolol
blockers with ISA acebutol
blockers labetalol, carvedilol
cardio non-selective:
blockers metiprolol, propranolol,
nadolol
blockers with ISA pindolol, bopindolol
- Penggunaannya terbatas
- methyldopa hypertension saat kehamilan
- methyldopa menyebabkan gejala pusing dan kelelahan
Adverse effects:
A) DIRECT ACTING
Minoxidil
- Membuka kanal kalium
- Lebih berefek pd arteriol dibanding pd vena
- Adverse: oedemas, hypertrichosis, breast tenderness
3. Vasodilators
Diazoxide
- Membuka kanal kalium
- adverse: Na+ and water retention, hyperglycaemia, hirsutism
Hydralazine
- arteriolar resistance
- Bermanfaat untuk hypertensive crisis selama kehamilan
- AE: Na+ and water retention, systemic lupus erythematosus
Indikasi :