Drug Monograph: Angiotensin II Receptor Antagonist
1
Drug Monograph: Angiotensin II Receptor Antagonist
Drug
Trade name3, 6
กลุ่มของยา
(ตามบัญชียาหลักแห่งชาติ )1
บริ ษทั ผู้ผลิ ต3, 6
Classification
Dosage form3, 6
ความแรง3, 6
ขนาดบรรจุ 1 กล่อง (tablet) 3, 6
ราคา (บาท/เม็ด) 3
Mechanism of action2, 4
Losartan
Irbesartan
Valsartan
Candesartan
cilexetil
Telmisartan
Olmesartan
medoxomil
COZAAR®
APROVEL®
DIOVAN®
BLOPRESS®
MICARDIS®
OLMETEC®
ค
(เฉพาะ 50 mg)
NED
NED
NED
NED
NED
MERCK
SHARP&DOHME
SANOFI AVENTIS
NOVARTIS
TAKEDA LTD
Film-coat tablet
Tablet
Film-coat tablet
Tablet
Tablet
Film-coat tablet
50 mg
150 mg, 300 mg
80 mg, 160 mg, 320 mg
8 mg, 16 mg
40 mg
20 mg, 40 mg
50 mg:
บรรจุ 30 เม็ด
150 mg:
บรรจุ 28 เม็ด
300 mg:
บรรจุ 28 เม็ด
BOEHRINGER
INGELHEIM
Angiotensin II Receptor Antagonist (Angiotensin II Receptor blocker)
80 mg: 2x14 = 28
(2 แผง แผงละ 14 เม็ด)
160 mg: 2x14 = 28
(2 แผง แผงละ 14 เม็ด)
320 mg: 4x7 = 28
(4 แผง แผงละ 7 เม็ด)
160 mg: 22.59 บาท/เม็ด
8 mg:
บรรจุ 28 เม็ด
16 mg:
บรรจุ 28 เม็ด
50 mg:
150 mg:
16 mg:
21.97 บาท/เม็ด
19.69 บาท/เม็ด
20.78 บาท/เม็ด
300 mg:
21.55 บาท/เม็ด
A selective and competitive, nonpeptide angiotensin II receptor antagonist
4x7 = 28
(4 แผง แผงละ 7 เม็ด)
80 mg:
23.62
PFIZER
20 mg:
บรรจุ 28 เม็ด
40 mg:
บรรจุ 28 เม็ด
20 mg: 17.12 บาท/เม็ด
40 mg: 26.22 บาท/เม็ด
แถมอีก 15% (22.79)
Drug Monograph: Angiotensin II Receptor Antagonist
Drug
Indication
USFDA Approval 4
Non-USFDA Approval 4
Losartan
Irbesartan
 Hypertension
 Hypertension
 Diabetic
 Diabetic
nephropathy
nephropathy
 Cerebrovascular
accident, In
hypertensive
patients with left
ventricular
hypertrophy;
Prophylaxis
 Cardiovascular
 Atrial fibrillation
event risk,
(Class IIb, Category
Reduction (Class
B)
IIa, Category B)
 Congestive heart
 Congestive heart
failure (Class IIb,
failure (Class IIa,
Category B)
Category B)
 Left ventricular
 Left ventricular
hypertrophy (Class
hypertrophy (Class
IIb, Category B)
IIb, Category B)
Valsartan
Candesartan
cilexetil
Telmisartan
 Hypertension
 Hypertension
 Congestive heart
failure
 Myocardial infarction
 Hypertension
 Heart failure
 Diabetic
nephropathy (Class
IIa, Category B)
 Left ventricular
hypertrophy (Class
IIb, Category B)
 Cerebrovascular
Congestive heart
accident; Prophylaxis
failure (Class III,
(Class IIb, Category
Category B)
B)
Left ventricular
 Diabetic nephropathy
hypertrophy (Class
(Class IIa, Category
IIb, Category B)
B)
 Left ventricular
hypertrophy
(Class IIb, Category
B)
2
Olmesartan
Medoxomil
 Hypertension
Drug Monograph: Angiotensin II Receptor Antagonist
Drug
Losartan
3
Irbesartan
Valsartan
Candesartan
cilexetil
Telmisartan
Olmesartan
Medoxomil
2 hours
2 hours
2 - 4 hours
within 3 hours
1 week
6 hours
3 – 6 hours
4 - 6 hours
6 - 8 hours
-
2 - 4 weeks
3 - 6 weeks
2 - 4 weeks
clinical response within
2 weeks
-
-
6-8 hr
Multiple Dose: 24 hr
25%
Single Dose: at least 24 hr
Single Dose: at least 24 hr
Multiple Dose: up to 7 days
25%-35%
 clinical response in
1 - 2 week
 Control of blood
pressure is
sustained more
than one year
Single Dose: 24 hr
Multiple Dose: 24 hr
60%-80%
15%
42%
24 hr
Multiple Dose: 24 hr
26%
No
No
40%-48% in AUC
No
No
No
98.7%
90%
94%-95%
> 99%
> 99.5%
99%
34 L
53-93 L
17 L
0.13 L/kg
500 L
15-40 L
Pharmacokinetic 4
Onset (hours): Antihypertensive, oral
 Initial Response:
Antihypertensive, oral
 Peak Response:
Antihypertensive, oral
 Maximal effect
Duration (hours):
Hypertension
Absorption
(Bioavailability)
Food interactions
Distribution
 Protein Binding
 Volume of distribution
Multiple Dose:
24 hr
Single Dose:
Multiple Dose:
24 hr
Single Dose:
Drug Monograph: Angiotensin II Receptor Antagonist
Drug
Metabolism
Prodrug
Active metabolite
Elimination: fecal
Elimination: urinary
Elimination half-life
(hours)
Contraindication 4
Precaution 4
4
Losartan
Irbesartan
Valsartan
Candesartan
cilexetil
Telmisartan
Olmesartan
Medoxomil
Liver, 14%
(CYP450-2C9 and
3A4)
-
Liver, 50%-70%
(CYP450 2C9)
Hepatic metabolism
Intestinal wall cell
(CYP450-2C9)
liver, less than 3%
conjugation
De-esterification
-
-
Candesartan cilexetil
-
Olmesartan
EXP 3174
-
-
Candesartan
-
Olmesartan
60%
80%
83%
67%
97%
50-65%
35%
20%
13%
33%
< 1%
35-50%
1.5-2
11-15
6-9
3.5-4
24
13
 angioedema
 aortic, mitral valve,
or renal artery
stenosis
 concomitant use
with an ACE
inhibitor and a betablocker is not
recommended in
CHF patients
 geriatric patients
75 years or older
with heart failure
 heart failure
 hepatic or renal
impairment
 hyperkalemia
 congestive heart
failure, severe
 dialysis
 hepatic impairment
or biliary obstructive
disorder
 renal artery
stenosis, unilateral
or bilateral
 renal impairment
 angioedema
 excessive hypotension
- volume-depletion
 hyperkalemia
 renal artery stenosis
 severe CHF




แพ้ยา
หญิงมีครรภ์
angioedema
excessive
hypotension volume-depletion
 hepatic or renal
impairment
 hyperkalemia
 renal artery
stenosis
 angioedema
 excessive
hypotension
 hepatic or renal
impairment
 hyperkalemia
 hypertrophic
cardiomyopathy
Drug Monograph: Angiotensin II Receptor Antagonist
Drug
Losartan
Irbesartan
 severe CHF
Adverse Reactions4, 5
Cardiovascular
 Chest pain 12%
 hypotension 7%
Central nervous system  Fatigue 14%
 Dizziness 4%
Endocrine
 Hyperkalemia
1-7%
 Hypoglycemia
14 %
Valsartan
Candesartan
cilexetil
Telmisartan
 excessive
hypotension volume-depletion
 hepatic or renal
impairment
 hyperkalemia
 severe CHF
 surgery/anesthesia
 Volume- and/or
salt-depleted
patients
 volume depletion
 Orthostatic
hypotension 5%
 hypotension 6-7%
 Postural hypotension
2%
 hypotension 19%
 Fatigue 4%
 Dizziness 10%
 Fatigue 2-3%
 Dizziness 2-17%
 Dizziness
 headache
 Chest pain 1%
 hypotension 1%
 Peripheral edema
1%
 headache 1%
 Dizziness 1%
 Fatigue 1%
 Hyperkalemia 19%  Hyperkalemia <1-2%
 Hyperkalemia <1-6%
5
Olmesartan
Medoxomil
 Dizziness 3%
 Hyperglycemia
 hypertriglyceridemia
Drug Monograph: Angiotensin II Receptor Antagonist
Drug
Gastrointestinal
Hematologic
Neuromuscular and
skeletal
Respiratory
Pregnancy category 4
Breast feeding 4
Losartan
 Diarrhea 2-15%
 Gastritis 5%
 Anemia 14%
Irbesartan
 Diarrhea 3%
 Dyspepsia 2%
 Weakness 14%
 Back pain 2-12%
 Cough: similar to
placebo
 Cough: similar to
placebo
Valsartan
Candesartan
cilexetil
Telmisartan
6
Olmesartan
Medoxomil
 Diarrhea 5%
 Abdominal pain 2%
 Neutropenia 2%
 Dyspepsia
 Gastritis
 Diarrhea 3%
 Dyspepsia 1%
 Diarrhea
 Back pain 3%
 Arthralgia 3%
 Back pain
 Weakness
 Back pain 3%
 Myalgia 1%
 Back pain
 CPK increased
 Upper respiratory
infection 7%
 Rhinitis
 sinusitis
 Cough 3%
 Dyspnea
 rhiitis
Category C (1st Trimester)
Category D (2nd Trimester)
Category D (3rd Trimester)
Infant risk cannot be ruled out
Drug Monograph: Angiotensin II Receptor Antagonist
Reference
1. คณะกรรมการแห่งชาติดา้ นยา. บัญชียาหลักแห่งชาติ พ.ศ. 2551 (แก้ไขเพิม่ เติมครัง้ ที3่ ). 2008;[79 screens].
Available at: URL:http://wwwapp1.fda.moph.go.th/ed2547/ed-list.asp Accessed May 16, 2009.
2. สมชาย เอีย่ มอ่อง, สุรพันธ์ สิทธิสขุ และสมเกียรติ. Angiotensin II Receptor Blocker. พิมพ์ครัง้ ที่ 1. Text and Journal Publication Co. Ltd. Bangkok 2546.
3. ศูนย์ขอ้ มูลข่าวสารด้านเวชภัณฑ์ กระทรวงสาธารณสุข ราคาอ้างอิ งของยาเดือนตุลาคม-ธันวาคม 2551. 2008 [160 screens].
Available at: http://www.dmsc.moph.go.th Accessed May 16, 2009.
4. Klasco RK (ed): DRUGDEX® System. Thomson Micromedex, Greenwood Village, Colorado (Edition expires March 2009).
5. Lacy,C.F., Armstrong,L.L., Goldman,M.P. & Lance,L.L. Drug Information Handbook International with Canadian and International Drug monographs. 14th
ed. Ohio: Lexi-Comp, Inc.; 2006.
6. Romano MB. ed. MIMS Thailand 1st Issue 2008. 104th ed. Bangkok: TIMS (Thailand) Ltd; 2008:55-56.
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