Transcript Antiandrenergic agents- peripherally acting

Antianginal Agents and
Hypotensive Agents
馬偕紀念醫院藥劑室
林育成藥師
Amlodipine besylate (Norvasc)
• Form: Tab:5mg
• Dosage:
– Hypertension: Initial 2.5-5mg qd, MD 5-10mg
qd, Max. 10mg/day
– Angina: 5-10mg qd, MD 10mg qd
Amlodipine besylate (Norvasc)
• Precautions
– aortic stenosis
– CHF
– exacerbation of angina during initiation of
therapy, after dose increases, or withdrawal of
beta blocker therapy
– hypotension (initially or after dose increases)
– liver impairment
– persistent progressive dermatologic reactions
Amlodipine besylate (Norvasc)
• Dose adjustments:
• renal impairment: NOT recommended in
patients with severe renal impairment (CrCl
below 30 mL/min/1.73m(2), serum
creatinine >/=3 mg/dL)
• liver disease: starting dose, 2.5 mg/10 mg
• geriatrics: starting dose, 2.5 mg/10 mg
Isosorbide dinitrate (Isordil,
Sorbitrate tab, Isoket inj)
• Dose:
– Oral, initial 5-20 mg q6h, MD 10-40mg q6h ac,
– IV infusion, 2-7mg/hr, up to 10mg/hr
• Note:
– Dosing interval may be bid or tid and last dose
no later than 7 PM to minimize nitrate tolerance
Isosorbide mononitrate
(Imdur CR)
• Form: Tab: 60mg (extended release)
• Dose:
– Initial 30mg qd for 2-4 days then 60-120 mg
qd
• Note:
– should be taken in the morning
– should be swallowed whole not chewed, but it
can be administered half of a tablet at a time
Isosorbide monotrate (ISMO-20,
Isormol)
• Form: Tab:20mg
• Dose:
– Initial 10mg bid for 2 days then 20-30mg bid
• Note:
– Asymmetrical dosing regimen of 7AM and
3PM or 9AM and 5PM to allow for a nitratefree dosing interval to minimize nitrate
tolerance
– Do not crush or chew but can cut half
Isosorbide monotrate (ISMO-20,
Isormol)
• Administration:
• administer 0.5 hr before or 1 hr after meals
• do not crush or chew extended release
dosage forms
• dose to provide a 10-12 hr drug-free interval
Drug-drug interaction:
Organic nitrate and Sildenafil (Viagra)
• SILDENAFIL inhibits phosphodiesterase type 5
(PDE5) which is responsible for the metabolic
degradation of cyclic guanosine monophosphate
(cGMP).
• Organic nitrates exert their action by activation of
guanylate cyclase, which increases cGMP.
Because of the potential for excessive hypotensive
effects as a result of increased cGMP, the
concomitant use of sildenafil and organic nitrates
is contraindicated
Diltiazem HCl (Herbesser, Cartil)
• Form: Tab:30mg
• Dose:
– angina: start with 30mg qid ac, increase dosage
gradually until optimal response, average 180360 mg/ day divide into 3-4 doses
Diltiazem HCl (Diltelan SR)
• Form: Cap: 90mg (controlled release)
• Dose: Initial 90mg bid for 2 wks, may
increase gradually to 360mg/day div. into 2
dose
– Hypertension: 240-360mg/day
– Angina: 240mg/day
• Note: Swallow whole; do not open, chew or
crush the capsules
Nicorandil (Sigmart)
• Form: Tab:5mg
• Dose: 5-20 mg bid, Max. 30mg bid
Mechanism of Nicorandil
(Sigmart)
• Nicorandil : potassium channel openers or
activators, which produce vascular smooth muscle
relaxation by increasing potassium flux through
adenosine triphosphate (ATP)-sensitive
sarcolemmal potassium channels
• This leads to hyperpolarization of the cell
membrane, and subsequent decreases in levels of
cytoplasmic calcium (calcium channel blockade)
and dilation of arterial resistance vessels
Nifedipine (Adalat OROS)
• Form: Tab:30 mg (extended release)
• Dose: initial 30mg once daily, may be
increased to 120mg once daily if needed
• Note: Swallow whole; do not crush or chew
Nitroglycerin (Glyceryl trinitrate,
NTG, Nitrostat tab, Tridil inj)
• Form: Tab:0.6mg, inj:50 mg/10ml amp
• Dose:
– Sublingal, 0.2-0.6mg every 5 min for max. of 3
doses in 15 min
– IV infusion, initial 5mcg/min then increased by
5mcg/min at 3-5 min intervals until a response
is noted or the rate is 20mcg/min
Nitroglycerin lingual aerosol
• Form: Aerosol: 0.4mg/spray, 200 sprays/set
• Dose:
– Acute relief of angina pectoris: 1-2 srpays (0.40.8mg) every 3-5min if necessary , Max. of 3
doses in 15 min
– Prophylaxis angina pectoris: 1-2 sprays, 510min before situations
Antiadrenergic agents-centrally
acting
• Clonindine HCl (Catapres)
• Methyldopa (Aldomet)
12.06A ACE Inhibitors
Captopril
Enalapril
maleate
商品名 Capoten
Form
Tab: 25mg
Dose
Initial 25mg
bid-tid ac, the
dosage being
increased to
50mg bid-tid
if necessary
for 1 or 2 wks
FDA
[C] 1ST
class
trimester
[D] 2nd and 3rd
trimester
Fosinopril
Sodium
Renitec
Tab: 4mg
Initial 2.5mg
/day, MD 1040mg/day div.
into 1-2 doses
Monopril
Tab:10mg
Initial 10mg
qd, MD 2040mg/day qd
or bid up to
80mg/day
Perdindopril
(tertbutylamine)
Acertil
Tab:4mg/day
Initial 2 mg
qd, MD
4mg/day,
Max. 8mg/day
ac
[C]/[D]
[C]/[D]
[C]/[D]
Ramipril
Tritace
Cap:2.5mg
Initial 1.252.5mg qd, MD
2.5-5mg as a
single dosage
or in 2 divided
doses. Max.
10mg/day
[C]/[D]
Captopril (Capoten)
• Form: Tab:25mg
• Dose: Hypertension : Initial mg bid-tid ac,
the dosage being increased to 50mg bid-tid
if necessary after 1 or 2 wks
CHF: Initial 25mg tid ac, the dosage being
increased up to 50mg tid; if further
increased in dosage, it is made after an
interval of 2 wks, MD 50-100mg bid-tid,
Max. 450mg/day
Cotraindication of Capoten
• A. Angioedema induced by other angiotensin
converting enzyme (ACE) inhibitors during prior
exposure
• B. Anuric renal failure during prior exposure to
ACE inhibitors
• C. Hypersensitivity to this or any other ACE
inhibitor
• D. Hereditary or idiopathic angioedema
• E. Pregnancy (second and third trimesters
particularly
Enalapril maleate (Renitec)
• Form: Tab:20mg
• Dose:
– Hypertension: Initial 2.5~5mg/day, MD 1040mg/day divide into 1-2 doses
– CHF: initial 2.5mg qd-bid, MD 5-20mg/day
divide into 1-2 doses, Max. 40mg/day
Enalapril maleate (Renitec)
• MECHANISM :
• Enalapril is a weak angiotensin-converting
enzyme inhibitor; however, hepatic
activation of enalapril to enalaprilat being
10 to 20 times as potent as captopril
Enalapril maleate (Renitec)
• Precautions:
• ACE-inhibitor induced angioedema
• apheresis (low-density lipoprotein) with
dextran sulfate
• CHF, severe (oliguria and/or progressive
azotemia may occur)
Fosinopril Sodium (Monopril)
• Form: Tab: 10mg
– Hypertension: initial 10mg qd, MD
20~40mg/day qd or bid up to 80mg/day
– CHF: initial 10mg qd, MD 20~40mg/day
Fosinopril Sodium (Monopril)
• Mechanism :
• Fosinopril is a prodrug and must undergo
reesterification to its biologically active
diacid metabolite, fosinoprilat. Fosinopril
has a phosphinic acid binding site and lacks
the sulfhydryl group characteristic of
captopril
Fosinopril Sodium (Monopril)
• Precautions
– ACE-inhibitor induced angioedema
– apheresis (low-density lipoprotein) with
dextran sulfate
– CHF, severe (oliguria and/or progressive
azotemia may occur)
– collagen vascular disease, especially in
presence of renal impairment (risk of
neutropenia, agranulocytosis)
Perindopril tert-butylamine
(Acertil)
• Form: Tab: 4mg
• Dose:
– Hypertenision: Initial 2mg qd, MD 4mg/day,
Max. 8mg/day, Max. 8mg/day ac
CHF: Initial 2mg qd, MD 4mg/day ac
Perindopril tert-butylamine
(Acertil)
• Mechanism:
• Perindopril is an ester prodrug, requiring in
vivo hydrolysis to its active diacid
metabolite, perindoprilat
• Perindoprilat is a long-acting, non-thiol
angiotensin converting enzyme (ACE)
inhibitor
Rampril (Tritace)
• Form: Cap: 2.5mg
• Dose:
Hypertension: initial 1.25-2.5mg qd, MD
2.5-5mg as a single dosage or in 2 divided
doses. Max. 10mg/day
CHF post-MI: initial 2.5mg bid, if
hypotension occurs,dosage should be
reduced to 1.25mg bid. MD 5mg bid
Rampril (Tritace)
• Mechanism :
• Ramipril is a prodrug that undergoes
enzymatic saponification by esterases in the
liver to its biologically active metabolite,
ramiprilat. Ramipril is a long active
angiotensin converting enzyme inhibitor
with hypotensive effects lasting a full 24
hours with single daily dosing.
12.06 B Antiadrenergic Agents-Centrally Acting
Clonidine HCl
Methyldopa
Aldomet
商品名 Catapres
Form Tab:75mcg
Tab:250mg
Dosage Initial 0.05-.01mg bid,
Initial 250mg bid-tid for 2 days
may be increase by 0.1- then being adjusted until the
0.2mg/day, MD 0.2desired response is obatined,
0.12mg/day div. Into 2-4 MD 500mg-2g/day div. Into 2doses, Max. 2.4mg/day
4 doses
ADR
CNS depression,
Liver damage, fever, Coombsorthostasis, localized
positive hemolytic anemaia
reactions, dry mouth
Clonidine (Catapres)
• Form: Tab:75mcg
• Dose:
– Initial 0.05-0.1mg bid, may be increase by 0.10.2 mg/day,
– MD 0.2-1.2mg/day divide into 2-4 doses,
– Max. 2.4mg/day
Methyldopa (Aldomet)
• Form: Tab:250mg
• Dose:
– Initial 250mg bid-tid for 2 days then being
adjusted until the desired response is obtained,
– MD 500mg-2g/day divide into 2-4 doses
12.06 C Antiadrenergic agents-peripherally acting
Alfuzosin Doxazosin
Terazosin
HCl
商品 Xatral XL
名
Form Tab: 10mg
(prolong
release)
Dose Benign
prostatic
hyperplasia
:10mg qhs
Doxaben
Hytrin
Tab: 1mg
Form: 2mg
Initial 1mg qd, MD 2mg qd, if
necessary subsequent dosage
adjustments can be made by
doubling the dose every 2
wks, Max. 16mg/day
Hypertension: Initial 1mg hs, may
be increased gradually to 5mg/day,
Max. 20mg/day
Benign prostatic hyperplasia:
Initial 1mg hs, may be increased
in a stepwise manner to 2 to 5 and
10mg/day as necessary, Max.
20mg/day
Alfuzosin HCl (Xatral XL)
• Indication:
– Benign prostatic
hyperplasia
• Form: Tab:10mg
(prolonged release)
Alfuzosin HCl (Xatral XL)
• A. Alfuzosin: a selective -1 adrenoceptor
antagonist.
• B. dosing information:
– benign prostatic hyperplasia :7.5 to 10 mg daily;
– hypertension, 5 to 10 mg twice daily.
• Dose reductions are suggested in patients
with liver disease, and in the elderly.
Alfuzosin HCl (Xatral XL)
•
CONTRAINDICATIONS
• A. Concomitant use of potent CYP3A4 inhibitors
(eg, ketoconazole, itraconazole, ritonavir)
• B. Hepatic insufficiency (moderate to severe)
• C. Hypersensitivity to alfuzosin or other
quinazolines
Alfuzosin HCl (Xatral XL)
• Precautions:
• A. Carcinoma of the prostate and benign prostatic
hyperplasia may cause the same symptoms and
frequently coexist. Prostate cancer should be ruled
out prior to treatment.
• B. Concomitant use of other alpha-blockers
• C. Congenital or acquired QT prolongation
syndromes
• D. Coronary artery disease
Alfuzosin HCl (Xatral XL)
•
•
•
•
•
•
•
Precautions:
E. General anesthesia
F. Hepatic disease (mild)
G. Dizziness, lightheadedness
H. Orthostatic hypotension
I. Renal dysfunction (severe)
J. Syncope (First-dose effect)
Doxazosin (Doxaben)
• Indications
– Benign prostatic hyperplasia
– Hypertension
• Form: Tab: 1mg
• Dose: Initial 1mg qd, MD 2mg qd, if
necessary subsequent dosage adjustments
can be made by doubling the dose every 2
wks, Max. 16mg/day
Doxazosin (Doxaben)
• Precautions
• carcinoma of the prostate
• concomitant use of other antihypertensives
(additive hypotensive effects)
• first dose syncope/ sudden loss of consciousness
• liver disease
• orthostatic hypotension, syncope
• recent cerebrovascular accident
Doxazosin (Doxaben)
• Administration
• first dose phenomenon characterized by
excessive postural hypotension, palpitations,
syncope, and tachycardia can be minimized
by limiting the initial dose to 1 mg,
administering the first dose at bedtime, and
increasing the dosage slowly
Terazosin
• Form: Tab: 2mg
• Dose:
– Hypertension: Initial 1mg hs, may be increased
gradually to 5mg/day, Max. 20mg/day
– Benign prostatic hyperplasia: Initial 1mg hs,
may be increased in a stepwise manner to 2,5
and 10mg/day as necessary, Max. 20mg/day
12.06 D Antiadrenergic Agents-Beta-Adrenergic Blockers
Acebutolol
Atenolol Betax Bisoprolol Esmolol HCl
olol furamate
HCl
1
1
1
1
1
分類
Tenormi Kerlo Concor 5 Brevibloc
商品名 Sectral
n
ne
Form Tab: 400mg Tab:
Tab: Tab: 5mg Inj:100mg/10 ml
50mg
20mg
vial
Dose
Hypertension: Initial 50 102.5-20mg Intra-OP and
(Hyper- 400mg/day, mg qd, 40mg qd, Max. post-OP
tension) optimal
may
qd
20 mg/day tachycardia and
response
increase
hypertension:
usually 400- to
LD, IV 80mg
800mg/day 100mg/d
over 30 sec,
ay
followed by IV
infusion150
mcg/kg/min
Propranolol
HCl
1，2
Inderal,
Cardiolol
Tab: 10mg
Initial 20-40
mg bid, usual
dosage 160480mg/day
Acebutolol Hydrochloride
(Sectral)
• Angina: 600-1600 mg ORALLY daily (divided 23 times/day)
• Arrhythmias: initial, 400 mg ORALLY daily
(divided twice a day); maintenance, 600-1200 mg
ORALLY daily (divided 2-3 times/day)
• Hypertension: initial, 400 mg ORALLY daily;
maintenance, 400-800 mg ORALLY daily (may be
divided twice a day); MAX 1200 mg/day (divided
twice a day)
Acebutolol Hydrochloride
(Sectral)
• Dose Adjustments
• geriatric: may require lower maintenance
doses (specific guidelines unavailable);
doses above 800 mg/day should be avoided
• renal impairment: CrCl less than 50 mL/min
- reduce usual adult dose by 50%
• renal impairment: CrCl less than 25 mL/min
- reduce usual adult dose by 75%
Acebutolol Hydrochloride
(Sectral)
• FDA labeled indications
– Arrhythmia
– Hypertension
• Non-FDA labeled indications
– Angina pectoris
Acebutolol Hydrochloride
(Sectral)
• Contraindications
–
–
–
–
–
cardiogenic shock
hypersensitivity to acebutolol
overt cardiac failure
second and third degree AV block
severe sinus bradycardia
Atenolol (Tenormin)
• Form: Tab: 50mg
• Hypertension (HTN): 50-100 mg ORALLY
once daily
Atenolol (Tenormin)
• Dose Adjustments:
• hemodialysis: 25-50 mg after each dialysis
session
• renal impairment: CrCl 35 mL/min or
greater - normal dosing
• renal impairment: CrCl 15-35 mL/min MAX dose 50 mg once daily
• renal impairment: CrCl less than 15 mL/min
- MAX dose 25 mg once daily
Atenolol (Tenormin)
• Contraindications
–
–
–
–
–
cardiogenic shock
hypersensitivity to atenolol
overt cardiac failure
second and third degree AV block
severe sinus bradycardia
Atenolol (Tenormin)
• Precautions(1):
•
•
•
•
•
•
anesthesia/surgery (myocardial depression)
avoid abrupt withdrawal
bronchospastic disease
congestive heart failure
diabetes mellitus
hyperthyroidism/thyrotoxicosis
Atenolol (Tenormin)
• Precautions(2):
• patients receiving clonidine - discontinue atenolol
several days prior to withdrawal of clonidine
• peripheral vascular disease
• pregnancy
• renal impairment
Betaxolol HCl (kerlone)
• FDA labeled indications
– Glaucoma/Ocular hypertension
– Hypertension
• Non-FDA labeled indications
– Angina pectoris
Betaxolol HCl (kerlone)
• Dosage, Adult (usual)
• Angina: 5-80 mg once daily
• Glaucoma/ocular hypertension: 1-2 drops
(0.25% suspension) twice daily
• Hypertension: initial, 10 mg once daily,
maintenance, 10-40 mg once daily
Bisoprolol fumarate (Concor 5)
• Form: Tab: 5mg
• Dosage:Dosage, Adult (usual)
• Angina: 5-20 mg once daily
• CHF: initial, 1.25 mg once daily, titrate to
maximum dose of 10 mg once daily
• HTN: initial, 2.5-5 mg once daily, maintenance,
2.5-20 mg once daily, maximum dose, 40 mg once
daily
Bisoprolol fumarate (Concor 5)
• Dose adjustment:
•
•
•
•
•
hemodialysis: dose replacement is not necessary
liver disease: initial, 2.5 mg once daily
liver disease: maximum dose, 10 mg once daily
renal impairment: initial, 2.5 mg once daily
renal impairment: maximum dose, 10 mg once
daily
12.06E Antiadrenergic agent-Alpha/Beta-Adrenergic Blockers
Carvedilol
Laberalol HCl
112
112
分類
Trandate
商品名 Dilatrend
Form Tab: 6.25mg,
Tab: 200mg, Inj:25mg/5ml amp
25mg
Dosage Hypertension:
Oral, initial 100mg bid; may increase
Initial 6.25mg bid as needed every 2-3 days by 100mg
for 1-2 wks, then bid until desired response is obatined;
increased to
MD, 200-400 mg bid, Max. 2-4g/day
12.5mg bid, Max. IV, 20 mg over 2 min , additional
50mg/day
40mg or 80 mg may be given at 10
min intervals until the desired BP is
achieved or to a total dose of 300mg
Infusion, 200 mg is added to 160-250
ml of IV fluid administered at rate of
2mg/ min, the dosage is adjusted
according to BP response
Carvedilol (Dilatrend)
• Form: Tab: 6.25mg, 25mg
• Dose:
– Hypertension: Initial 6.25mg bid for 1-2 wks,
then increased to 12.5mg bid, Max. 50mg/day
Carvedilol (Dilatrend)
• Dose Adjustments:
• hemodialysis: dosing adjustments are NOT
required
• liver disease: initial, 20% of the normal
dose
Carvedilol (Dilatrend)
• FDA labeled indications
– Congestive heart failure
– Hypertension
– Postmyocardial infarction with left ventricular
dysfunction
• Non-FDA labeled indications
– Angina pectoris
Carvedilol (Dilatrend)
• Contraindications
• bronchial asthma or chronic obstructive
pulmonary disease
• cardiogenic shock
• hypersensitivity to carvedilol
• overt cardiac failure
• second and third degree AV block
• severe liver failure
• severe sinus bradycardia
• sick sinus syndrome
Labetalol HCl (Trandate)
• Indications
• FDA labeled indications
– Hypertension
• Non-FDA labeled indications
– Angina pectoris
Labetalol HCl (Trandate)
• Dosage:
• Oral, initial 100mg bid; may increase as needed
every 2-3 days by 100mg bid until desired
response is obtained; MD, 200-400 mg bid, Max.
2-4g/day
• IV, 20 mg over 2 min , additional 40mg or 80 mg
may be given at 10 min intervals until the desired
BP is achieved or to a total dose of 300mg
• Infusion, 200 mg is added to 160-250 ml of IV
fluid administered at rate of 2mg/ min, the dosage
is adjusted according to BP response
Calcium channel blocking agents
• 1.Benzothiazepine gr.
• 2. Didydropyridine gr.
• 3. Phenylalkylamine gr.
12.06 F Calcium Channel Blocking Agents
Amlodipine
Diltiazem HCl
besylate
2
1
分類
Norvasc
Diltelan SR
商品名
Form
Tab: 5mg
Tab: 90mg
Dosage
Felodipine
2
Plendil
Tab: 5mg
(extended
release)
Hypertension: Initial 90mg bid Hypertension:
Initial 2.5-5mg for 2wks, may Initial 5mg qd,
qd, MD 5-10 qd, increase
MD 5-10mg qd,
Max, 10mg/day gradually to
Max. 20mg qd
Angina: 5-10mg 360mg/day div.
qd, MD 10mg Into 2 doses
qd
Hypertension:
240-360mg/day
Isradipine
2
DynaCirc SRO
Cap: 5mg
(substained
release)
Initial, 5mg qd,
may be adjusted
in increments of
5mg/day at 24wks intervals,
Max. 20mg/day
12.06 F Calcium Channel Blocking Agents (2)
Nicardipine HCl Nimodipine
Perdipine
Nimotop
商品名
分類
Form
Dosage
Verapamil HCl
Isoptin,
Verpamil
2
2
3
Inj: 10mg/10ml, Inj: 0.2mg/ml, Tab:40mg;
amp
50 ml/vial
Inj: 5mg/2ml
amp
IV infusion,
Neurological
Hypertension:
initial 5mg/h,
deficit following oral, initial
may be
subarachnoid
80mg bid; MD
increased by
hemorrhage: IV 360-480 div.
2.5mg/h every infusion, initial Into 3-4 doses
15min up to a 1mg/h for 2 hrs Angina: Oral,
max. 15mg/h, then increased initial 80mg bid;
may be
to 2mg/h; if
MD 360increased by
patients <70kg 480mg/day
2.5mg/h every or with unstable
15min up to a BP, INITIAL
Max. 15mg/,
DOSE
MD 3mg/h
<0.5mg/h,
infusion should
be continued for
at least 5 days
and no more
than 14 days
Nimodipine (Nimotop)
• Form: Inj: 0.2mg/ml, 50ml/vial
• Dose:Neurological deficits following
subarachonoid hemorrhage: IV infusion,
initial 1mg/h for 2hrs then increased to
2mg/h; if patients<70kg o r with unstable
BP, initial dose<0.5mg/h, infusion should be
continued for at least 5 days and nor more
than 14 days/
Isardipine (Dynacirc SRO)
• Form: Cap: 5mg (sustained release)
• Dose: Initial, 5mg qd, may be adjusted in
increasements of 5mg/day at 2-4 wks
intervals, Max. 20mg/day
• Note: swallow whole
Felodipine (Plendil)
• Form: Tab: 5mg (extended release)
• Hypertension: initial 5mg qd, MD 5-10mg
qd, Max. 20mg qd
• Note: Swallow whole; do not crush or chew
Hydralazine HCl (Apresoline,
Aprezin)
• Form: Tab: 10mg, 50mg, Inj: 20mg powder
in amp
• Dose: oral: initial 10mg qid for the first 2-4
days then increased by 10-25mg with meals,
Max. 300mg/day divide into 4 doses
• IM, slow iv, 20-40mg
Hydralazine HCl (Apresoline,
Aprezin
• Contraindication:
• A. Previous hypersensitivity to hydralazine,
dihydralazine, or cadralazine
• B. Dissecting aortic aneurysm
Hydralazine HCl (Apresoline,
Aprezin
• Precautions
•
•
•
•
A. Coronary artery disease
B. History of cerebrovascular disease or stroke
C. Renal insufficiency
D. Hydralazine-induced systemic lupus
erythematosus
Hydralazine HCl (Apresoline,
Aprezin
• Precautions:
• E. Resulting peripheral neuropathy may be related
to pyridoxine deficiency.
• F. Hydralazine may reduce the pressor responses
to epinephrine.
• G. Apresoline(R) tablets may contain FD+C
yellow 5 (tartrazine).
Minoxidil (Loniten)
• Form: Tab:10mg
• Dose; Initial 2.5-5mg qd, can be increased
at least 3 days intervals to 10,20 then 40mg
in single or divided doses; ususal dose 1040mg/day, Max. 100mg/day
Minoxidil (Loniten)
• Contraindications:
• hypersensitivity to minoxidil products
• pheochromocytoma (systemic use)
Minoxidil (Loniten)
•
•
•
•
Precautions:
angina pectoris (exacerbation)
cerebrovascular disease
concomitant use of guanethidine (profound
orthostatic effects)
• malignant hypertension
• may cause congestive heart failure (without
adequate diuretic therapy)
• myocardial infarction (recent)
12.06I Agents for hypertensive emergences
Nitroglycerin
藥名
商品名 Glyceryl trinitrage, NTG
Form
Inj: 50mg/10 ml
Dosage IV infusion: Initial 5mcg/min then
increased by 5mcg/min at 3-5 min
intervals until a response is noted or
the rate is 20mcg/min
Note
It should be preseved in tight glass
containers and special nitroglycerin
IV set ( non-PVC) should be used
Nitroprusside
Nipride
Inj: 50mg powder in vial
IV infusion (50mg in 250-1000ml of
D5W), 3mcg/kg/min (range: 0.310mcg/kg/min)
After the preparation of diluted
infusion solutiosn, the infusion
containers and the tubing should be
immediately wrapped int eh enclosed
aluminum foil to protect the infusion
solution from light
Nitroprusside sodium dihydrate
(Nipride)
• Form: inj. 50mg powder in vial
• Dosage: IV infusion (50mg in 250-1000ml
of D5W), 3mcg/kg/min (range:0.310mcg/kg/min)
• Note: protect from light
Dose Adjustment of Nitroprusside
• hepatic insufficiency: consideration should
be made for cyanide toxicity since cyanide
is converted to thiocyanate by the liver;
dosage adjustments may be required
(specific guidelines unavailable)
• renal impairment: nitroprusside's metabolite
thiocyanate accumulates during renal failure
and should be monitored to ensure levels
remain less than 10 mg/dL
Nitroprusside sodium dihydrate (Nipride)
•
•
•
•
•
PRECAUTIONS
A. Excessive hypotension
B. Cyanide toxicity
C. Methemoglobinemia
D. Pre-existing anemia and/or hypovolemia
12.06 J Angiotensin II receptor (type AT1)
Losartan
藥名 Irbesartan
Cozzar
商品 Aprovel
名
Form Tab: 150mg
Tab: 50mg
25-100mg/day
劑量 150 mg/ daily,
Max. dose
div. into 1-2 doses
300mg/day
ADR Diarrhea,
Headache,
dyspepsia/heart- hypertension,
burn, upper
methemoglobine
respiratory tract mia, cyanide
infection,
toxicity
headache, fatigue
telmisartan
Micardis
Valsartan
Diovan
Tab: 40mg
Initial 40mg/day;
usual dose 2080mg/day
Headache,
dizziness, cough
Tab: 80mg
80/day; may be
increased to
160mg if needed
Dizziness,
hypotension,
angioedema,
cough
Angiotensin II receptor (type AT1)
antagonist
• [C] 1st trimester; [D] 2nd and 3rd trimester
• Drugs acting directly on the renin-angiotensin- aldosterone
system are documented to cause fetal harm.
• ACE inhibitors may cause fetal or neonatal injury or death
when used during the second or third trimester of
pregnancy. Hypotension, neonatal anemia, hyperkalemia,
neonatal skull hypoplasia, anuria, and renal failure have
occurred in fetuses and neonates.
• Oligohydramnios  decreased fetal renal function,
• limb contractures, craniofacial deformities, and hypoplastic
lung development
Irbesartan (Aprovel)
• Form: Tab:150mg
• Dosage, adult (usual)
– Hypertension: 150 mg once daily, MAX 300
mg once daily
Irbesartan (Aprovel)
• contraindications
• A. Hypersensitivity to irbesartan
• B. Pregnancy
Losartan potassium (Cozzar)
• Form: Tab:50mg
• Dose:25-100mg/day divide into 1-2 doses
• FDA labeled indications
– Nephropathy, diabetic II patients with a history
of hypertension
– Hypertension
Losartan potassium (Cozzar)
•
•
•
•
•
•
•
Precautions:
angioedema (present or past)
excessive hypotension - volume-depletion
hepatic or renal impairment
hyperkalemia
renal artery stenosis
severe CHF
Telmisartan (Micardis)
• Form: Tab:40mg
• Dose: Initial 40mg once daily; usual dose
20-80 mg once daily
Telmisartan(Micardis)
• Contraindication:
• A. Hypersensitivity to telmisartan
• B. Pregnancy
Valsartan (Diovan)
• Form: Cap:80mg
• Dose: 80mg/day; may be increased to
160mg if needed
Valsartan (Diovan)
• Administration:
• may be administered without regard to food
• may be given with other antihypertensive
agents
• avoid potassium supplements or potassiumcontaining salt substitutes
Valsartan (Diovan)
• Precautions :
•
•
•
•
•
avoid lithium
electrolyte imbalance
hepatic or renal impairment
hyperkalemia
pregnancy
Valsartan (Diovan)
• Precautions:
• sensitivity reactions may occur with or
without a history of allergy or asthma
• systemic lupus erythematosus
• volume-/salt-depletion - excessive
hypotension