Antihypertensive Drugs-Cardiovascular Pharmacology抗高血压,心血管药理学

Calcium Channel Blockers
Dihydropyridines
Amlodipine Felodipine Nimodipine Isradipine Nicardipine Nifedipine
Non-Dihydropyridines
Bepridil Diltiazem Verapamil
ß-Adrenergic Antagonists (Beta Blockers)
Acebutalol (Sectral) Atenolol (Tenormin) Betaxolol (Kertone) Bisoprolol (Zebeta) Carteolol (Cartrol) Metoprolol (Lopressor)
Endocrine Diesease
◆ Adrenocortical hyperactivity (Cushing‘s disease, primary hyperaldosteronism) ◆ Oral contraceptives ◆ Pheochromcytoma ◆ Acromegaly ◆ Myxedema
Clonidine
Approved uses: – Treatment of hypertension – For severe pain in cancer patients
Clonidine
Unlabeled uses: – Alcohol withdrawal – Methadone/opiate detoxification – Smoking cessation facilitation
Neurogenic Disease
◆ Psychogenic ◆ Polyneuritis ◆ Elevated intracranial pressure ◆ Familial dysautonomia
Miscellaneous
◆ Increased intravascular volume ◆ Polyarteritis nodosa ◆ Hypercalcemia ◆ Aortic coarctation
As blood volume returning to the heart increases, preload increases and there is enhanced filling with ventricular dilation.
Heart rate:
Heart Rate X Stroke Volume = Cardiac Output
* Crosses membranes easily->α-CH3-DA-> αCH3-NE * Conversion occurs only in neurons and CNS
-Displaces NE from granules->NE metabolized by MAO -Higher affinity for presynaptic α2R -> ↓ NE release in vasomotor center -> ↓ TPR and ↓ BP -Is as potent as NE on periphal receptors
Penbutalol (Levatol) Pindolol (Visken) Propranolol (Inderal) Sotalol (Betapace) Timolol (Blocadren)
THANKS!
The sympathetic nervous system maintains arterial blood pressure by several mechanisms:
Sympathetic maintains BP
Long-Term Regulation
Anti-Hypertensive Drug Classes
Peripheral resistance:
For a given cardiac output, blood pressure depends only on peripheral resistance. Some antihypertensive drugs act to reduce peripheral resistance.
Diuretics Centrally Active Adrenergic Neuron Blocker Adrenoceptor Antagonists Vasodilators Calcium Channel Blockers Angiotensin Converting Enzyme Inibitors Angiotensin Receptor Blocker
Control of Blood Pressure
Physiological Factors Influencing Arterial Pressure
Preload & Contractility
Peripheral resistance
Heart Rate
Preload & Contractility
Mechanism of Antihypertension
Reduce preload
Reduce contractility
Reduce peripheral resistance
Antihypertension
Reduce afterload
Decrease heart rate
The basic regulating mechanism of short period arterial blood pressure is baroreceptors. When the blood pressure is elevated, the baroreceptors is stimulated. It can inhibit vasoconstrictor center through oblongata solitary tract, and stimulate vagus nerve center. The results are that peripheral vasorelaxation, myocardial negative tension effect and negative rhythm effect.
– Atrial fibrillation – Diabetic diarrhea – Reduction of allergen-induced inflammatory reactions in patients with extrinsic
α-methyldopa :
Enters the synthesis pathway at the DOPA step
Unknown Etiology
◆ Toxemia of pregnancy ◆ Acute intermittant porphyria ◆ Essential Hypertension (> 90% of all cases of hypertension）
Essential Hypertension
Cardiovascular Pharmacology
Antihypertensive Drugs
Classification of Arterial Hypertension
Systolic hypertension
Systolic and Diastolic
hypertension
Renal Disease
Essential hypertension occurs in patients who have arterial hypertension without a clear, definable cause.
Also referred to Primary or idiopathic hypertension.
Adrenergic Neuron Blocker
Guanethidine Reserpine
Adrenoceptor Antagonists
Labetalol (alpha & beta) Prazosin (alpha) Terazosin (alpha)
Vasodilators
Diazoxide Hydralazine Minoxidil Nitroprusside sodium
Angiotensin Converting Enzyme Inhibitors (ACEI)
Benazepril Captopril Enalapril Fosinopril Quinapril Ramipril
Angiotensin Receptor Blocker
Saralasin Losartan Irbesartin
Endocrine Disease
Miscellaneous
Etiology
Unknown Etiology
Neurogenic Disease
Renal Disease
◆ Renovascular stenosis or renal infarction ◆ Polycystic kidney disease ◆ Acute and chronic glomerulonephritis ◆ Chronic pyelonephritis ◆ Renin-producing tumors ◆ Other severe renal diseases
Cardiac Output X Peripheral Resistance = Arterial Pressure
Since the product of Fra Baidu bibliotekeart rate and stroke volume equals cardiac output, an increase
in heart rate will increase arterial blood pressure, all other factors remaining equal.
Centrally Active
Clonidine Methyldopa Guanabenz Guanfacine
α2-Adrenergic Agonist
• clonidine • major action is in the brain (tends to
overrideaction in the periphery) – decrease sympathetic tone – sedative effect at higher doses