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Blood Pressure мм
stage
Systolic Diastolic
Normal 101-139 61-89
Boundary Hypertens. 140-159 90-94
160-179 95-109
I stage – mild
(functional, transint) No sings of infringement of
target organs
II stage – moderate 180-199 110-119
(initial systemic Hypertrophy of the LV,
infringement, labile) constriction of retina arteria
etc.
III stage – hard > 220 > 120
(systemic organic Disturbance of the cerebral,
infringement, permanent) coronary, renal blood flow
REGULATION OF BLOOD PRESSURE
capacity work of the pump
venules heart
CNS
resistance sympathetic n.s.
volume
arterioles kidneys
renin
aldosteron angiotensin
ANTIHYPERTENSIVE AGENTS
neurotropic:
tranquilizers,
on sympathetic neuroleptics,
transmission: psychosedatives
central 2-adrenomimetics (clonidine,
methyldopa)
selective agonist of imidazoline
receptors (moxonidin)
- & β-adrenoblockers
sympatholytics
on water- ganglioblockers
salt
balance miotropic
diuretics, ACE (vasodilators):
inhibitors, nonselective (papaverin, no-spa
antagonists of etc), selective (Са2+-channels
angiotensin II blockers, К+-channels activators
receptors etc)
CENTRAL 2-ADRENOMIMETICS
clonidine (clophelin), methyldopa,
guanfacin
peripheral resistance (more in upright
position)
heart beat and cardiac output (more in
horizontal position)
prevent left ventricle hypertrophy and heart
failure
dilation of the cerebral, renal and cardiac
blood vessels
renin and aldosterone production
sedative, analgesic effects
adverse effects:
drowsiness, constipation, dryness of mouth, initial
hypertension (I.V.), bradycardia etc.
rebound syndrome, pseudotolerance, alcohol
potentiation
EFFECTS OF BETA-BLOCKERS
block of β- sympathetic block of
receptors of nervous system cardiac β-
renal juxta- receptors
glomerular zone
cardiac
contractility
and rate
cardiac
renin excitability
secretion and
cardiac conductivity
output
peripheral
vessels tonus myocardial
oxygen
demand
therapeutic uses:
hypertension
ischemic heart disease
arrhythmia - drugs with MSA
glaucoma - timolol
hyperthyroidism – propranolol
migraine, alcohol abstinence – propranolol
β-BLOCKERS
Adverse effects
cariovascular: arrhythmia (АV-block, bradycardia
etc), heart failure, hypotension, edema
bronchospasm
vasoconstriction («claudication»)
hypoglycemica
LDLP
“down-regulation” of beta-receptors
rebound syndrome with tachycardia
pregnant uterus contraction
MIOTROPIC (VASODILATORS)
Na+ retention,
BP cardiac
blood volume output
1 – diuretics 2 – β-blockers
MIOTROPIC (VASODILATORS)
non-selective:
phosphodiesterase inhibitors:
isoquinolone derivative – papaverin, no-
spа (drotaverin)
xanthine derivative – theophyllin,
aminophyllin (euphyllin)
mixed mechanism of action – apressin
(hydralazine), diabzol, nicotinic acid etc.
selective:
Ca2+- channels blockers – nifedipine,
verapamil, diltiazem
K+-channels openers – minoxidil,
diazoxide
nitrous oxide donators – sodium
nitroprusside
CALCIUM CHANNEL BLOCKERS
Type I (cardiotropic) –phenylalkylamines
derivatives : verapamil and others.
Са2+
Сa2+- + calmodulin
channels
blockers Сa2+ + calmodulin
kinase of light kinase of
miosin chanes - light miosin
Сa2+ РО4 chanes
miosin (non- miosin - РО4
ATP-
aza active) (active)
+ actin
contraction
EFFECTS OF Ca 2+ CHANN. BLOCKERS
heart vessels
conductive myocardium coronary peripheral
system
AV-node SA-node contractility dilation
resistance
Coronary blood
flow
Arterial BP
Heart rate
AV-conductivity -
CALCIUM CHANNELS BLOCKERS
therapeutic uses:
hypertension
infringement of cerebral blood flow, migraine
(nimodipine, cinnarizine)
Paynaud’s phenomenon (amlodipine)
ischemic heart disease
supraventricular tachyarrhythmia (verapamil,
diltiazem)
adverse effects:
arrhythmia: bradycardia, АV-block etc.
(verapamil, diltiazem)
hypotension, reflective tachycardia
heart failure, edema
redness of skin, dizziness, headache,
constipation etc.
POTASSIUM CHANNELS OPENERS
MInoxidil, diazoxide
К+-channels opening
К+ outflux
hyperpolarization
block of voltage-gated
Сa2+- channels
Сa2+ intracellular influx
smooth muscles tonus
vasodilation
BP
POTASSIUM CHANNELS OPENERS
therapeutic uses:
alternative agents for hypertension:
severe hypertension, resistant to other agents
(minoxidil)
hypertonic crisis (diazoxide)
Ischemic heart disease: variant angina
(nicorandil)
adverse effects:
adverse effects
hypotension (initial doses)
infringement of kidneys function
(proteinurea)
hyperkaliemia
edema
dry cough
dermal allergic reactions (10 % of patients)
embryotoxic
PHARMACODYNAMICS OF
ANGIOTENSIN-RECEPTOR BLOCKING
AGENT
peripheral resistance & BP ( after-load)
systolic & diastolic BP
heart rate, hypertrophy of left ventricular
angioprotective action
sodium & uric acid excretion
aldosterone, NA, A production
renin, angiotensin I & II level (negative
feedback)
unlike ACE inhibitors:
don’t alter bradykinin, prostaglandins and
potassium level in blood
less prominent adverse effects
HYPERTONIC CRISIS (EMERGENCY)
Route of Onset of Duration of
Agents admini action (min) action (hrs)
stration
Sodium I.V. Beginning of End of
nitroprusside infusion infusion
Diazoxide I.V. 1-5 1-12
Hydralazine I.V. 5-10 4-6
Subling. 15-30 3-6
Nifedipine
I.V. 1-5 3-6
Labetolol I.V. 1-5 6-24
also available:
furosemide (lazix) I.V.
neurotropic – diazepam (I.V.), amizine (I.V.,
I.M.), magnesium sulfate (I.V.) etc.
CLASSIFICATION OF HYPETENSIVE
AGENTS
adrenomimetics – adrenalin, ephedrine,
noradrenalin, mesaton, dobutamine, dopamine
glucocorticoids – prednisolone,
dexamethasone
mineralocorticoids – DOCSA
analeptics – caffeine, cordiamine,
sulfocamphocaine
adaptogens – Ginseng, Eleuterococ,
Echinacea etc