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Agent Adrenergic
Receptor
Blocking
Activity
Lipid
Solubility
Protein
Bound
(%)
Half-
Life
(h)
Bioavail-
ability
(%)
Primary
(Secondary)
Route of
Elimination
Indications Usual
Dosage
Acebutolol
(Sectral®)
beta1 Low 15-25 3-4 40
7-fold1
Hepatic
(renal)
Hypertension, arrhythmias P.O.: 400-
1200 mg/d
Atenolol
(Tenormin®)
beta1 Low <5-10 6-92 50-60
4-fold1
Renal
(hepatic)
Hypertension, angina
pectoris, acute MI
P.O.: 50-200
mg/d
I.V.: 5 mg x
2 doses
Betaxolol
(Kerlone®)
beta1 Low 50-55 14-22 84-94 Hepatic
(renal)
Hypertension P.O.: 10-20
mg/d
Bisoprolol
(Zeneca®)
beta1 Low 26-33 9-12 80 Renal
(hepatic)
Hypertension, heart failure P.O.: 2.5-5
mg
Carteolol
(Cartrol®)
beta1
beta2
Low 20-30 6 80-85 Renal Hypertension P.O.: 2.5-10
mg/d
Carvedilol
(Coreg®)
beta1
beta2
alpha1
ND 98 7-10 25-35 Bile into feces Hypertension, heart failure
(mild to severe)
P.O.: 6.25
mg twice
daily
Esmolol
(Brevibloc®)
beta1 Low 55 0.15 NA
5-fold1
Red blood cell Supraventricular
tachycardia, sinus
tachycardia
I.V.
infusion: 25-
300
mcg/kg/min
Labetalol
(Normodyne®
, Trandate®)
alpha1
beta1
beta2
Moderate 50 5.5-8 18-30
10-fold1
Renal
(hepatic)
Hypertension P.O.: 200-
2400 mg/d
I.V.: 20-80
mg at 10-
min
intervals up
to a
maximum of
300 mg or
continuous
infusion of 2
mg/min
Metoprolol
(Lopressor®,
Toprol-XL®)
beta1 Moderate 10-12 3-7 50
10-fold1
(Toprol
XL®: 77)
Hepatic/renal Hypertension, angina
pectoris, acute MI, heart
failure (mild to moderate;
XL formulation only)
P.O.: 100-
450 mg/d
I.V.: Post-
MI 15 mg
Angina: 15
mg then 2-5
mg/hour
Arrhythmias
: 0.2 mg/kg
Nadolol
(Corgard®)
beta1
beta2
Low 25-30 20-24 30
5- to 8-
fold1
Renal Hypertension, angina
pectoris
P.O.: 40-320
mg/d
Penbutolol
(Levatol®)
beta1
beta2
High 80-98 5 100 Hepatic
(renal)
Hypertension P.O.: 20-80
mg/d
Pindolol beta1
beta2
Moderate 57 3-42 90
4-fold1
Hepatic
(renal)
Hypertension P.O.: 20-60
mg/d
Propranolol
(Inderal®,
various)
beta1
beta2
High 90 3-52 30
20-fold1
Hepatic Hypertension, angina
pectoris, arrhythmias
P.O.: 40-480
mg/d
I.V.: Reflex
tachycardia
1-10 mg
Propranolol
long-acting
beta1
beta2
High 90 9-18 20- to 30-
fold1
Hepatic Hypertrophic subaortic
stenosis, prophylaxis (post-
P.O.: 180-
240 mg/d
(Inderal-
LA®)
MI)
Sotalol
(Betapace®,
Betapace
AF®,
Sorine®)
beta1
beta2
Low 0 12 90-100 Renal Ventricular arrhythmias/
tachyarrhythmia
P.O. 160-
320 mg/d
Timolol
(Blocadren®)
beta1
beta2
Low to
moderate
<10 4 75
7-fold1
Hepatic
(renal)
Hypertension, prophylaxis
(post-MI)
P.O.: 20-60
mg/d
P.O.: 20
mg/d
Dosage is based on 70 kg adult with normal hepatic and renal function.
Note: All beta1-selective agents will inhibit beta2 receptors at higher doses.
1Interpatient variations in plasma levels.
2Half-life increased to 16-27 hours in creatinine clearance of 15-35 mL/minute and >27 hours in creatinine clearance <15 mL/minute.
# Chief
complia
nt
Past
medical
Hx.
Past
surg.
Hx.
Social Hx.
(tobacco)
(alcohol)
Lab.investigation Final
Dx.
Tx. Clinical
outcome
Blood
sugar
Blood
urea
Serum
electrolyt
es
Lipid
profile
both
TG &
cholest
erol
Serum
troponin
PCV
ESR
1 Chest
pain
-ve Penfort
al DV
+ve
(heavy
smoker),
-ve alc
normal normal normal MI Metoprol
ol 50mg
Still in
hospital
2 Chest
pain
- ve -ve -ve, -ve normal high normal
ESR
Unstable
angina
Metoprol
ol 50 mg
Still in
hospital
3 Chest
pain
Hyperte
nsion on
capoten
tab25
-ve +ve
(heavy
smoker, -
ve alc.
normal normal high +ve normal
PCV &
ESR
IHD
Acute
coronar
y synd.
Metoprol
ol 25 mg
improve
4 Chest
pain
IHD -ve +ve
(heavy
smoker, -
ve alc.
normal
+ve
low
ESR
Acute
coronar
y synd.
STEMI
Metoprol
ol 50 mg
improve
5 Chest
pain
Hyperte
nsion on
lovasc
2.5
-ve -ve, -ve
alc.
normal MI Metoprol
ol 50 mg
improve
6 Shortnes
s of
breath
Hyperte
nsion on
Inderal
Hrenio
rrhaph
y &
-ve, -ve normal Low
PCV
AF Propranol
ol 40 mg
improve
40 catarac
t
7 Chest
pain
Hyperte
nsion on
amlodipi
n|+ IHD
on
isordil
-ve -ve, -ve normal normal -ve normal
PCV
Pulmon
ary
oedema
Atenolol
50 mg
Still in
hospital
8 Epigastr
ic pain
-ve -ve -ve, -ve high +ve high
ESR
antiSTE
MI
cardioge
nic
shock
Metoprol
ol 50 mg
dead
9 Chest
pain
hyperte
nsion
-ve -ve, -ve normal normal -ve Low
PCV
Unstable
angina
Metoprol
ol 50 mg
improve
10 Chest
pain
Hyperte
nsion
5years
& DM
on
insulin
-ve +ve
(heavy
smoker), -
ve
high +ve low
ESR
angina Metoprol
ol 50 mg
improve
11 epigastri
a pain
DM on
oral
hypogly
cemic
agent
-ve -ve, -ve normal normal low normal ectopic
SVT
Metoprol
ol 50 mg
improve
12 unconsci
ous
hyperte
nsion
when he
tonsil
surger
y
-ve, +ve
alc
high Na
normal K
alc.
intoxific
ation &
Atenolol
(p.m.hx)
Still in
hospital
was 31
year
drug
poison -
ing
13 CVA left
side for
CT of
brain
CVA left
side,
hyperte
nsion on
Tenormi
n
-ve -ve, -ve normal low Na
low K
low
PCV
Atenolol
(p.m.hx)
Still in
hospital
14 leg pain,
CRF
hyperte
nsion on
Tenormi
n, DM
on
metform
in
-ve -ve, -ve normal high Na
high K
CRF Atenolol
(p.m.hx)
Still in
hospital
15 anorexia
&
abd.pain
CRF,
hyperte
nsion
renal
transpl
antatio
n
-ve, -ve normal high low Na
normal K
anorexia Timolol
(p.m.hx)
Still in
hospital
16 vomiting DM on
glibencl
amide,
rheumat
ism,
hyperte
nsion on
Tenormi
n
-ve -ve, -ve high Atenolol
(p.m.hx)
Still in
hospital
17 disturbe
d
concentr
ation
CRF &
hyperte
nsion on
furosemi
de &
Tenormi
n
nephro
ctomy,
pertoni
al
dialysis
-ve, -ve normal normal normal
Na
high K
Atenolol
(p.m.hx)
Still in
hospital
18 chest
pain
hyperte
nsion on
tenormi
n-1year
-ve -ve, -ve high normal normal
Na
low K
high normal
PCV
angina Atenolol
(p.m.hx)
Still in
hospital
19 vomiting
&
diarrhea
hyperte
nsion on
Tenormi
n
-ve -ve, -ve Atenolol
(p.m.hx)
Still in
hospital
20 right
upper
abdomin
al pain
hyperte
nsion at
2006,
psoriasis
-ve -ve, -ve normal normal gall
bladder
stone
Bisoprolol
(p.m.hx)
Still in
hospital
21 loss of
consciou
s
MI since
5years
ago
herniac
tomy
&
vascula
r surg.
-ve, -ve metoprolo
l 20 mg
improve
22 hematoe
mesis
-ve -ve, -ve low jaundice
,
enlarged
spleen
propranol
ol 40 mg
improve
Evaluation of beta blockers in Iraqi hospital-tables

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Evaluation of beta blockers in Iraqi hospital-tables

  • 1. Agent Adrenergic Receptor Blocking Activity Lipid Solubility Protein Bound (%) Half- Life (h) Bioavail- ability (%) Primary (Secondary) Route of Elimination Indications Usual Dosage Acebutolol (Sectral®) beta1 Low 15-25 3-4 40 7-fold1 Hepatic (renal) Hypertension, arrhythmias P.O.: 400- 1200 mg/d Atenolol (Tenormin®) beta1 Low <5-10 6-92 50-60 4-fold1 Renal (hepatic) Hypertension, angina pectoris, acute MI P.O.: 50-200 mg/d I.V.: 5 mg x 2 doses Betaxolol (Kerlone®) beta1 Low 50-55 14-22 84-94 Hepatic (renal) Hypertension P.O.: 10-20 mg/d Bisoprolol (Zeneca®) beta1 Low 26-33 9-12 80 Renal (hepatic) Hypertension, heart failure P.O.: 2.5-5 mg Carteolol (Cartrol®) beta1 beta2 Low 20-30 6 80-85 Renal Hypertension P.O.: 2.5-10 mg/d Carvedilol (Coreg®) beta1 beta2 alpha1 ND 98 7-10 25-35 Bile into feces Hypertension, heart failure (mild to severe) P.O.: 6.25 mg twice daily Esmolol (Brevibloc®) beta1 Low 55 0.15 NA 5-fold1 Red blood cell Supraventricular tachycardia, sinus tachycardia I.V. infusion: 25- 300 mcg/kg/min Labetalol (Normodyne® , Trandate®) alpha1 beta1 beta2 Moderate 50 5.5-8 18-30 10-fold1 Renal (hepatic) Hypertension P.O.: 200- 2400 mg/d I.V.: 20-80 mg at 10- min intervals up
  • 2. to a maximum of 300 mg or continuous infusion of 2 mg/min Metoprolol (Lopressor®, Toprol-XL®) beta1 Moderate 10-12 3-7 50 10-fold1 (Toprol XL®: 77) Hepatic/renal Hypertension, angina pectoris, acute MI, heart failure (mild to moderate; XL formulation only) P.O.: 100- 450 mg/d I.V.: Post- MI 15 mg Angina: 15 mg then 2-5 mg/hour Arrhythmias : 0.2 mg/kg Nadolol (Corgard®) beta1 beta2 Low 25-30 20-24 30 5- to 8- fold1 Renal Hypertension, angina pectoris P.O.: 40-320 mg/d Penbutolol (Levatol®) beta1 beta2 High 80-98 5 100 Hepatic (renal) Hypertension P.O.: 20-80 mg/d Pindolol beta1 beta2 Moderate 57 3-42 90 4-fold1 Hepatic (renal) Hypertension P.O.: 20-60 mg/d Propranolol (Inderal®, various) beta1 beta2 High 90 3-52 30 20-fold1 Hepatic Hypertension, angina pectoris, arrhythmias P.O.: 40-480 mg/d I.V.: Reflex tachycardia 1-10 mg Propranolol long-acting beta1 beta2 High 90 9-18 20- to 30- fold1 Hepatic Hypertrophic subaortic stenosis, prophylaxis (post- P.O.: 180- 240 mg/d
  • 3. (Inderal- LA®) MI) Sotalol (Betapace®, Betapace AF®, Sorine®) beta1 beta2 Low 0 12 90-100 Renal Ventricular arrhythmias/ tachyarrhythmia P.O. 160- 320 mg/d Timolol (Blocadren®) beta1 beta2 Low to moderate <10 4 75 7-fold1 Hepatic (renal) Hypertension, prophylaxis (post-MI) P.O.: 20-60 mg/d P.O.: 20 mg/d Dosage is based on 70 kg adult with normal hepatic and renal function. Note: All beta1-selective agents will inhibit beta2 receptors at higher doses. 1Interpatient variations in plasma levels. 2Half-life increased to 16-27 hours in creatinine clearance of 15-35 mL/minute and >27 hours in creatinine clearance <15 mL/minute.
  • 4. # Chief complia nt Past medical Hx. Past surg. Hx. Social Hx. (tobacco) (alcohol) Lab.investigation Final Dx. Tx. Clinical outcome Blood sugar Blood urea Serum electrolyt es Lipid profile both TG & cholest erol Serum troponin PCV ESR 1 Chest pain -ve Penfort al DV +ve (heavy smoker), -ve alc normal normal normal MI Metoprol ol 50mg Still in hospital 2 Chest pain - ve -ve -ve, -ve normal high normal ESR Unstable angina Metoprol ol 50 mg Still in hospital 3 Chest pain Hyperte nsion on capoten tab25 -ve +ve (heavy smoker, - ve alc. normal normal high +ve normal PCV & ESR IHD Acute coronar y synd. Metoprol ol 25 mg improve 4 Chest pain IHD -ve +ve (heavy smoker, - ve alc. normal +ve low ESR Acute coronar y synd. STEMI Metoprol ol 50 mg improve 5 Chest pain Hyperte nsion on lovasc 2.5 -ve -ve, -ve alc. normal MI Metoprol ol 50 mg improve 6 Shortnes s of breath Hyperte nsion on Inderal Hrenio rrhaph y & -ve, -ve normal Low PCV AF Propranol ol 40 mg improve
  • 5. 40 catarac t 7 Chest pain Hyperte nsion on amlodipi n|+ IHD on isordil -ve -ve, -ve normal normal -ve normal PCV Pulmon ary oedema Atenolol 50 mg Still in hospital 8 Epigastr ic pain -ve -ve -ve, -ve high +ve high ESR antiSTE MI cardioge nic shock Metoprol ol 50 mg dead 9 Chest pain hyperte nsion -ve -ve, -ve normal normal -ve Low PCV Unstable angina Metoprol ol 50 mg improve 10 Chest pain Hyperte nsion 5years & DM on insulin -ve +ve (heavy smoker), - ve high +ve low ESR angina Metoprol ol 50 mg improve 11 epigastri a pain DM on oral hypogly cemic agent -ve -ve, -ve normal normal low normal ectopic SVT Metoprol ol 50 mg improve 12 unconsci ous hyperte nsion when he tonsil surger y -ve, +ve alc high Na normal K alc. intoxific ation & Atenolol (p.m.hx) Still in hospital
  • 6. was 31 year drug poison - ing 13 CVA left side for CT of brain CVA left side, hyperte nsion on Tenormi n -ve -ve, -ve normal low Na low K low PCV Atenolol (p.m.hx) Still in hospital 14 leg pain, CRF hyperte nsion on Tenormi n, DM on metform in -ve -ve, -ve normal high Na high K CRF Atenolol (p.m.hx) Still in hospital 15 anorexia & abd.pain CRF, hyperte nsion renal transpl antatio n -ve, -ve normal high low Na normal K anorexia Timolol (p.m.hx) Still in hospital 16 vomiting DM on glibencl amide, rheumat ism, hyperte nsion on Tenormi n -ve -ve, -ve high Atenolol (p.m.hx) Still in hospital
  • 7. 17 disturbe d concentr ation CRF & hyperte nsion on furosemi de & Tenormi n nephro ctomy, pertoni al dialysis -ve, -ve normal normal normal Na high K Atenolol (p.m.hx) Still in hospital 18 chest pain hyperte nsion on tenormi n-1year -ve -ve, -ve high normal normal Na low K high normal PCV angina Atenolol (p.m.hx) Still in hospital 19 vomiting & diarrhea hyperte nsion on Tenormi n -ve -ve, -ve Atenolol (p.m.hx) Still in hospital 20 right upper abdomin al pain hyperte nsion at 2006, psoriasis -ve -ve, -ve normal normal gall bladder stone Bisoprolol (p.m.hx) Still in hospital 21 loss of consciou s MI since 5years ago herniac tomy & vascula r surg. -ve, -ve metoprolo l 20 mg improve 22 hematoe mesis -ve -ve, -ve low jaundice , enlarged spleen propranol ol 40 mg improve