1.

Obat anti hipertensi

a. Diuretik
Dengan cara menghambat transfer NaCl di tubulus ginjal dan meningkatkan
eksresi sodium
Hidroklorotiazid 12.5mg, 25mg tab, dosis harian 6.25 50mg, 1-2x/hari.
b. ACE Inhibitor
Mencegah perubahan angiotensin I menjadi angiotensin II sehingga terjadi
vasodilatasi dan penurunan sekresi aldsteron, melakukan degradasi bradikinin
yang juga menurunkan tensi.
Captopril 12.5, 25mg tab, dosis harian 25 100mg, 2-3x/hari.
c. Angiostensin II Renin sistem bloker (ARB)
ARB akan menghambat vasokonstriksi dengan cara menghambat
pembentukan atau kerja dari Angiotensin II, sehingga menyebabkan
vasodilatasi yang berimbang.
Valsartan 80mg, 160mg tab, dosis harian 80 320mg, 1-2x/hari.
d. Beta bloker
Menurunkan frekuensi denyut jantung dan kontraktilitas miokard sehingga
curah jantung menurun. Mengahambat sekresi renin di sel justaglomerulus
ginjal sehingga penurunan kadar angiotensin. Pada sentral terjadi efek
penurunan aktivitas saraf simpatik.
Bisoprolol 5mg tab (selektif), dosis harian 20mg/hari, 1x/hari
Propanolol (non selektif) 10mg, 40mg tab, dosis harian 40-160mg, 2-3x/hari
e. Calcium Antagonist (CCB)
Menghambat influx kalsium pada sel di otot polos, pembuluh darah, jantung
sehingga terjadi relaksasi arteriol dan resistensi perifer menurun dan tensi
menurun
Amlodipine 5mg, 10mg tab, dosis harian 5 -10mg, 1x/hari
Nifedipine 10mg, dosis harian 30 60mg, 2-3x/hari
f. Alpha antagonis
Terjadi vasodilatasi arteriol dan venula kemudian menurunkan resistensi
perifer sehingga aliran balik ke vena menurun dan curah jantung menurun
Prazosin : 1mg, 2mg tab, dosis harian 0.5-4mg, 1-2x/hari
g. Alpha 2 agonis
Bekerja pada sentral, menurunkan resistensi perifer dengan menghambat
outflow simpatis sehingga dapat menurunkan tonus simpatis.
Metildopa : 250mg, dosis harian 250-500mg, 2x/hari.

TABlE
298-8

ExAMPlES oF oRAl DRugS uSED in TREATMEnT oF HYPERTEnSion

Drug Class
Diuretics

Usual Total Daily Dosea

Examples
(Dosing Frequency/Day)
Contraindications/Cautions

Other Indications

Thiazides

Hydrochlorothiazide
6.2550 mg (12)
Diabetes, dyslipidemia,
hyper- Chlorthalidone
uricemia, gout,
2550 mg (1)
hypokalemia
Loop diuretics
Furosemide
4080 mg (23)
CHF due to systolic dysfunc- Diabetes,
dyslipidemia, hyper- Ethacrynic acid
tion, renal failure
50100 mg (23)
uricemia, gout, hypokalemia
Aldosterone antagonists Spironolactone
25100 mg (12)
CHF due to systolic dysfunc- Renal failure,
hyperkalemia Eplerenone 50100 mg (12)
tion, primary aldosteronism

Beta blockers
Cardioselective
sick-

Atenolol

25100 mg (1)

Asthma, COPD, 2nd- or

Angina, CHF due to systolic 3rd-degree heart block,
dysfunction, post-MI, sinus sinus syndrome
tachycardia,
ventricular
tachyarrhythmias

Nonselective
Alpha antagonists
Selective

Nonselective
Sympatholytics
Central

ACE inhibitors

Angiotensin II antagonists

Renin inhibitors
Calcium antagonists
Dihydropyridines
Nondihydropyridines

Metoprolol
Propranolol
Propranolol LA

25100 mg (12)
40160 mg (2)
60180 (1)

Prazosin
Doxazosin
Terazosin
Phenoxybenzamine

220 mg (23)
116 mg (1)
110 mg (12)
20120 mg (23)

Clonidine
Clonidine patch
(1/week)
Methyldopa
Reserpine
Guanfacine
Captopril
bilateral Lisinopril
pregRamipril
Losartan
renal Valsartan
pregnancy,
Candesartan
Aliskiren

0.10.6 mg (2)
0.10.3 mg
2501000 mg (2)
0.050.25 mg (1)
0.52
mg
(1)(2)
25200
mg
1040 mg (1)
2.520 mg (12)
25100 mg (12)
80320 mg (1)
232 mg (12)
150300 mg (1)

Nifedipine (long-acting)
3060 mg (1)
Verapamil (long-acting)
120360 mg (12)
block Diltiazem (long-acting)

Prostatism

Pheochromocytoma

Post-MI, coronary syndromes, Acute renal failure,

CHF with low ejection frac- renal artery stenosis,
tion, nephropathy

nancy, hyperkalemia

CHF with low ejection frac- Renal failure, bilateral

tion, nephropathy, ACE inhibi- artery stenosis,
tor cough

hyperkalemia

Diabetic nephropathy

Pregnancy

Post-MI, supraventricular
180-420 mg (1)

2nd- or 3rd-degree heart

tachycardias, angina

2. Obat antihiperglikemia oral

a. Pemacu Sekresi Insulin (Insulin Secretagogue)
Sulfonilurea : Obat golongan ini mempunyai efek utama memacu sekresi
insulin oleh sel beta pankreas.
Obat

Dosis awal

Dosis

Pemberian

maksimal

sehari

Glibenklamid

2,5 mg

20 mg

1 - 2 kali ac

Gliklasid

80 mg

240 mg

1 - 2 kali ac

Glikuidon

30 mg

120 mg

2 - 3 kali

Glipisid

5 mg

20 mg

1 - 2 kali ac

Glimepirid

1 mg

8 mg

1 kali

b. Biguanid : peningkat Sensitivitas terhadap Insulin, mengurangi produksi

glukosa hati (glukoneogenesis), dan memperbaiki ambilan glukosa perifer.
Metformin 500mg, 850mg tab, dosis harian 500-2500mg, 1-3x/hari.
c. Tiazolidindion : merupakan agonis dari Peroxisome Proliferator Activated
Receptor Gamma (PPAR-), suatu reseptor inti termasuk di sel otot, lemak,
dan hati. Golongan ini mempunyai efek menurunkan resistensi insulin dengan
jumlah protein pengangkut glukosa, sehingga meningkatkan ambilan
glukosa di perifer.
Pioglitazine 15mg, 30mg tab, dosis harian 15-45mg, 1x/hari.
d. Penghambat Absorpsi Glukosa: Penghambat Glukosidase Alfa.
Obat ini bekerja dengan memperlambat absorbsi glukosa dalam usus halus,
sehingga mempunyai efek menurunkan kadar glukosa darah sesudah makan.
Acarbose 50mg, 10mg tab, dosis harian 25-300mg, 1-3x/hari
e. Penghambat DPP-IV (Dipeptidyl Peptidase-IV)
Obat golongan penghambat DPP-IV menghambat kerja enzim DPP-IV
sehingga GLP-1 (Glucose Like Peptide-1) tetap dalam konsentrasi yang
tinggi dalam bentuk aktif. Aktivitas GLP-1 untuk meningkatkan sekresi
insulin dan menekan sekresi glukagon bergantung kadar glukosa darah
(glucose dependent).
Sitagliptin 25mg, 50mg, 100mg, dosis harian 100mg, 1x/hari
Saxagliptin 2.5mg, 5mg tab, dosis harian 2.5-5mg, 1x/hari

TAblE
418-5

AgEnTS uSED foR TREATmEnT of TyPE 1 oR TyPE 2 DiAbETES

Mechanism
of Action

Examples

HbA1c
Reducti
on (%)b

AgentSpecific
Advantages

Oral
Biguanidesc

Hepatic glucose

Metformin

12

production

-Glucosidase inhibitorsc

GI glucose

Acarbose, miglitol,

absorption

voglibose

Dipeptidyl peptidase IV Prolong

endogenous
inhibitorsc
GLP-1
action

Insulin secretagogues:

Insulin secretion

Sulfonylureasc

Insulin secretagogues:

Insulin secretion

Nonsulfonylureasc
Thiazolidinedionesc

Alogliptin,

0.50.8
0.50.8

Serum creatinine

not cause hypogly- lactic acidosis

cemia, inexpensive,
extensive experience, CV events

>1.5 mg/dL (men)

>1.4 mg/dL (women)
(see text), CHF, radiographic contrast
studies,
hospitalized patients,
acidosis

Reduce
postprandial
glycemia

Renal/liver disease

GI flatulence, liver
function tests

Well tolerated, do

Reduced dose with

renal
disease; one associated

not cause hypoglycemia

Glibornuride, glicla- 12

Short onset of

zide, glimepiride,
glipizide, gliquidone,
glyburide,
glyclopyramide

action, lower post- weight gain

prandial glucose,
inexpensive

Nateglinide, repa-

0.51.0

Insulin resistance, Rosiglitazone,

pioglitazone
glucose

Contraindications

Weight neutral, do Diarrhea, nausea,

Anagliptin,
Gemigliptin, linagliptin, saxagliptin,
sitagliptin, teneligliptin, vildagliptin

glinide, mitiglinide

utilization

AgentSpecific
Disadvanta
ges

Short onset of

with increase heart

failure risk; possible
association with ACE inhibitor
induced angioedema
Hypoglycemia,

Renal/liver disease

Hypoglycemia

Renal/liver disease

Lower insulin

Peripheral edema,

CHF, liver disease

requirements

CHF, weight gain,

fractures, macular
edema

action, lower postprandial glucose

0.51.4

Proton Pump (H+,K+-ATPase) Inhibitors

Omeprazole, esomeprazole, lansoprazole, rabeprazole, and pantoprazole are substituted benzimidazole derivatives that covalently bind and irreversibly inhibit H+,K+-ATPase.
Esomeprazole, one of the newest members of this drug class, is the S-enantiomer of
omeprazole, which is a race- mic mixture of both S- and R-optical isomers. The R-isomer
of lansoprazole, dexlansoprazole, is the most recent PPI approved for clinical use.

Omeprazole and lansoprazole are the PPIs that have been used for the longest time. Both are
acid-labile and are administered as enteric-coated granules in a sustained-release capsule that
dissolves within the small intestine at a pH of 6. Lansoprazole is available in an orally
disintegrating tablet that can be taken with or without water, an advantage for individuals
who have significant dysphagia. In addition, a lansoprazole-naproxen combination
preparation that has been made available is targeted at decreasing NSAID-related GI injury.
Omeprazole is available as nonenteric-coated granules mixed with sodium bicarbonate in a
powder form that can be administered orally or via gastric tube. The sodium bicarbonate has
two purposes: to protect the omeprazole from acid degradation and to promote rapid gastric
alkalinization and subsequent proton pump activation, which facilitates rapid action of the
PPI.

Pantoprazole and rabeprazole are available as enteric-coated tablets. Pantoprazole is also

available as a parenteral formulation for intravenous use. These agents are lipophilic
compounds; upon entering the parietal cell, they are protonated and trapped within the acid
environment of the tubulovesicular and canalicular system. These agents potently inhibit all
phases of gastric acid secretion. Onset of action is rapid, with a maximum acid inhibitory
effect between 2 and 6 h after administration and duration of inhibition lasting up to 7296 h.

Sucralfate
Protects GI lining against peptic acid, pepsin and bile salt by binding with positively-charged
proteins in exudates forming a viscous paste-like adhesive substance thus forming a
protective coating.