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ANTIHYPERTENSIVE DRUGS
I. DIURETICS
Bumetanide, furosemide, hydrochlorthiazide, spironolactone, triamterene
II. -BLOCKERS
Atenolol, labetalol, metoprolol, propranolol, timolol
III. ACE INHIBITORS
Captopril, benazepril, enalapril, fosinopril, lisinopril, moexipril, quinapril,
ramipril
IV. ANGIOTENSIN II ANTAGONIST
Losartan
V. Ca++CHANNEL BLOCKERS
Amlodipine, diltiazem, felodipine, isradipine, nicardipine, nifedipine,
nisoldipine, verapamil
VI. -BLOCKERS
Doxazosin, prazosin, terazosin
VII. OTHER
Clonidine, diazoxide, hydralazine, -methyldopa, minoxidil, sodium
nitroprusside
TREATMENT STRATEGIES
Mild hypertension can often be controlled with a
single drug. More severe hypertension may
require treatment with several drugs that are
selected to minimize adverse effects of the
combined regimen. Treatment is initiated with
any of four drugs depending on the individual
patient: a diuretic, a -blocker, an ACE inhibitor,
or a calcium channel blocker. If blood pressure
is inadequately controlled, a second drug is
added. A -blocker is usually added if the initial
drug was a diuretic, or a diuretic is added if the
first drug was a -blocker. A vasodilator can be
added as a third step for those patients who still
fail to respond.
Oxodolin
(chlortalidon, hygroton)
Thiaside
diuretics
Peripheral vascular
resistance
Decreasing of arterial
pressure
Cardiac output
Hydrochlorothiazide+Losartan
Loop diuretics
The loop diuretics act promptly, even in
patients who have poor renal function or
who have not responded to thiazides or
other diuretics.
activation of
1-adrenoreceptors
of heart
Cardiac
output
Angiotensine
Renin
Aldosterone
Holding sodium
and water
Volume of
blood
circulation
Decreasing of
blood pressure
-adrenoblockers
Used for mostly mild to moderate cases of AH
(frequently in combinations with other drugs)
Stable hypotensive response develops over
1-3 weeks
Titration the effective dose. The -blockers may
take several weeks to develop their full effects
ACE-INHIBITORS
The angiotensin-converting enzyme (ACE)
inhibitors (captopril, enalapril, lisinopril,
perindopril) are recommended when the
preferred first-line agents (diuretics or blockers) are contraindicated or
ineffective.
MECHANISM OF ACTION OF
IACE
ANGIOTENSINOGEN
sympathetic
tone
Renin (kidneys)
ANGIOTENSIN
(inactive)
Decrease
angiotensine II
production
ACE
IACE
Decrease
aldosterone
production
peripheral
vessels tone
retention of
Na+ and H2O
bradicinine
Decrease of
arterial
pressure
Therapeutic uses
Like -blockers, ACE inhibitors are most
effective in hypertensive patients who are
white and young.
However, when used in combination with a
diuretic, the effectiveness of ACE inhibitors is
similar in white and black hypertensive patients.
ACE inhibitors are effective in the management
of patients with chronic congestive heart
failure.
ACE inhibitors are now a standard in the care of
a patient following a myocardial infarction.
Therapy is started 24 hours after the end of the
infarction.
ANGIOTENSIN II ANTAGONISTS
Losartan (Cozaar), Valsartan (Diovan),
Irbesartan (Avapro), Candesartan
(Atacand).
The nanopeptide losartan, a highly
selective angiotensin II receptor blocker,
has recently been approved for
antihypertensive therapy. Its
pharmacologic effects are similar to ACE
inhibitors in that it produces vasodilation
and blocks aldosterone secretion. Its
adverse effects is improved over the ACE
inhibitors, although it is fetotoxic.
ANGIOTENSIN II ANTAGONISTS
Verapamil
Dilthiasem
Niphedipin
Ischemic
heart disease
Verapamil
Dilthiasem
Niphedipin
Supraventricule
tachicardia
Verapamil
Dilthiasem
Possibility to
combine with
beta-blockers
recommended drug
Dilthiasem
Felodipin
Niphedipin
to use carefully
Amlodipin
Amlodipin
Felodipin
Amlodipin
Prasosine
( 1
adrenoblocker
adrenoblocker))
CENTRALLY-ACTING
ADRENERGIC DRUGS
CENTRALLY-ACTING
ADRENERGIC DRUGS
Adverse effects are generally mild, but the
drug can produce sedation and drying of
nasal mucosa. Rebound hypertension
occurs following abrupt withdrawal of
clonidine. The dug therefore should be
withdrawal slowly if the clinician wishes to
change agents.
CENTRALLY-ACTING
ADRENERGIC DRUGS
VASODILATORS
The direct-acting smooth muscle relaxants, such
as hydralazine and minoxidil, have traditionally
not been used as primary drugs to treat
hypertension. They act by producing relaxation
of vascular smooth muscle, which decreases
resistance and therefore decreases blood
pressure. These agents produce reflex
stimulation of the heart. They may prompt
angina pectoris, myocardial infarction, or cardiac
failure in predisposed individuals.
VASODILATORS
PRINCIPLES OF THERAPY
Therapeutic Regimens
Once the diagnosis of hypertension is established, a
therapeutic regimen must be designed and
implemented. The goal of management for most
clients is to achieve and maintain normal blood
pressure range (below 140/90 mm Hg). If this goal
cannot be achieved, lowering blood pressure to any
extent is still considered beneficial in decreasing the
incidence of coronary artery disease and stroke.
PRINCIPLES OF THERAPY
(contd)
If the initial drug (and dose) does not produce the desired
blood pressure, options for further management include
increasing the drug dose, substituting another drug, or
adding a second drug from a different group. If the
response is still inadequate, a second or third drug may
be added, including a diuretic if not previously
prescribed. When current management is ineffective,
reassess the clients compliance with lifestyle
modifications and drug therapy. In addition, review other
factors that may decrease the therapeutic response,such
as over-the-counter appetite suppressants, dietary or
herbal supplements, or nasal decongestants, which raise
blood pressure.
HYPERTENSIVE EMERGENCY
is a life-threatening situation in which the
diastolic blood pressure is either over 150
mm Hg (with systolic blood pressure
greater than 210 mm Hg) in an otherwise
healthy person, or 130 mm Hg in an
individual with preexisting complications,
such as encephalopathy, cerebral
hemorrhage, left ventricular failure, or
aortic stenosis. The therapeutic goal is to
rapidly reduce blood pressure.
Dose
0,5-10 mcg/kg/min (dropply)
Nitroglycerinum
Onset
immediately
Side effects
nausea, vomiting,
muscles, sweating
2-5 min
tachicardia,
vomiting,
fibrillation of
flushing,
headache,
Diazoxidum
50-100 mg (quickly)
300 mg (during 10 min)
2-4 min
nausea,
vomiting,,
hypotension,
tachicardia, flushing, redness of skin,
chest pain
Apressinum
10-20 mg
10 min
Furosemidum
2-3 min
hypotension, fatigue
Clophelinum
15-20 min
somnolence
Anaprilinum
20-30 min
bradicardia
Magnesium
sulfas
15-20 min
redness of skin
Labetololum
5-10 min
nausea,
dizzeness
vomiting,,
hypotension,
REFERENCES
http://www.escardio.org
http://www.cardiosmart.org
http://www.medscape.com/cardiology