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DRUGS
By Shabib Akhtar
NERVOUS SYSTEM
Includes neurons and ganglia outside of the brain and spinal cord
Peripheral Nervous System
Sympathomimetic drugs are substances that mimic the effects of the sympathetic nervous system, such as catecholamines, adrenaline (epinephrine), noradrenaline (norepinephrine), dopamine, etc.
Adrenaline
Ach (N) Adrenal medulla AUTONOMIC
Parasympathetic
Synapse
Ach (M) Smooth muscle Cardiac muscle
Ach (N)
Such drugs are used to treat cardiac arrest and low blood pressure, or even delay premature labor, among other things.
III. a)
Norepinephrine
b)
Phenylephrine
b)
Isoproterenol Selective 1
Dobutamine
II.
IV. a) b) c)
a)
Metaproterenol
b)
c) d)
Terbutaline
Salbutamol Ritodrine
V. a) b)
3. Mixed action: Combination of direct and indirect receptor stimulation, e.g. ephedrine and dopamine.
Stimulation of 2 receptors in CNS is useful in decreasing BP Most body tissues have both and receptors Effect occurs secondary to receptor activated and number of receptors in the particular body tissue Some drugs act on both receptorsdopamine
Pseudo Epinephrine
Isuprel (Isoproterenol): o Synthetic catecholamine that acts on 1 and 2 receptors o Stimulates heart, dilates blood vessels in skeletal muscle and causes bronchodilation o No alpha stimulation o Used in heart blocks (when pacemaker not available) and as a bronchodilator
Pharmacological properties Blockade of 1 adrenergic receptors inhibits the vasoconstriction produced by endogenous catecholamines. Blockade of 2 receptor present in the brain increases vasomotor tone. Block pressure action of adrenaline and causes fall in blood pressure. Vasomotor reversal of Dale. Reflex trachycardia and cardiac output. Blockade of 2 receptor- potentiate release of nor-epinephrine from adrenergic nerve ending. Blockade of 1 receptor mediated contraction of other smooth muscle.
II.
a) b) c)
d)
B.
Phenoxybnezamine:
Slow onset of action - ethyleneiumonium intermediate. Also block 5HT, histamine and acetylcholine responses. Action on cardiovascular system: blood pressure: postural hypotension. Heart: reflex trachycardia. Uses: in patient with pheochromacytoma.
Short duration of action Activation of cardiac adrenergic receptors. Activation of cholinergic receptors. Histamine like effect. Uses: to control hypertensive crisis, treatment of impotence in males. Tolazoline is used in treatment of presistent hypertension of the newborn.
Terazosin:
Less potent then prazosin. Has higher bioavailability. Have longer duration of action.
Uses:
Mild to moderate hypertension. Congestive heart failure. Conservative treatment of benign prostrate hypertrophy. Occasional postural hypotension and syncope.
ERGOT ALKALOIDS
Natural alkaloids
Ergotamine Ergotoxine: ergocristine+ ergocriptine+ ergocornine. Ergometrine (ergonovine)
Dihydrogenated alkaloid:
Dihydroergotamine. Hydergin.
Pharmacological actions:
-adrenergic receptor blockade. Smooth muscle stimulation. CNS excitation/depression.
Hydrogenation of ergot alkaloids increases- -blockade activity. Oxytocic effect : Ergonovine or ergotamine administered at second or third stage of labor. In migraine: ergotamine in combination with caffeine.
Pharmacological Action:
Cardiovascular system: Decreases both the force and rate of myocardial contraction as well as cardiac output. Produces slow developing hypotension. Pindolol with no plasma renin activity but effective antihypertensive. Respiratory tract: Bronchial constriction in asthmatic patient. Eye Decreases aqueous humor secretion. Metabolic effect: Beta-blocker inhibits the lipolytic and glycogenolytic action of catecholamines. Augment hypoglycemic action of oral hypoglycemics.
Cardiovascular system: fall in blood pressure- Fall in blood pressure is usually associated with bradycardia, decreased C.O and decrease pulse pressure.
Other effects: increases GIT motility, reduces I.O.P in glaucomatous eyes and produces difficulty or prevention of ejaculation. Therapeutic uses: Severe hypertension only after prior or simultaneous initiation of treatment with thiazide diuretics and reserpine.
RESERPINE
Mechanism of action: binds tightly to storage vesicles in adrenergic neurons destroying them and the nerve endings lose their ability to concentrate and store NE and dopamine. pharmacological action: Cardiovascular system: fall in blood pressure, reduces CO and peripheral resistance. Other effects: sedation, extra-pyramidal effects, increases GIT activity and nasal congestion. Therapeutic uses: use in treatment of hypertension.
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