pharmacological actions of epinephrine
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Slide 1 :
PHARMACOLOGICAL EFFECTS OF ADRENALINE (EPINEPHRINE) By Ibel .C. Fredy
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Adrenergic drugs (sympathomimetics) Direct sympathomimetics They directly act as agonists on alpha and beta receptors Eg:adrenaline,noradrenaline,phenylepinephrine,methoxamine,xylometazoline,salbutamol, Indirect sympathomimetics They indirectly acts on adrenergic neurons to release nor adrenaline which then acts on adrenergic receptors Eg:tyramine, amphetamine Mixed action sympathomimetics They act directly as well as indirectly Eg:ephedrine,dopamine,mephentermine
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MAJOR PHYSIOLOGICAL EFFECTS BY ADRENOCEPTOR AGONISTS SMOOTH MUSCLE NERVE TERMINALS HEART BLOOD VESSELS RESPIRATION EYE G.I.T URINARY BLADDER UTERUS C.N.S METABOLISM
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Smooth muscle CONTRACTION
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Nerve terminals Inhibition C.A release
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Heart +ve -Choronotrophy +ve- Ionotrophy
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Blood vessels Both vasoconstriction and vasodilatation can occur depending on the drug ,dose and vascular bed Constriction predominates in cutaneous ,mucous membrane, and renal beds By both alpha 1 and alpha 2 receptors Dilatation predominates in skeletal muscle, liver and coronaries
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Respiration Adrenaline and isoprenaline are potential vasodilators Adrenaline can directly stimulate R.C but this action is seldom manifest at clinically used doses
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EYE Adrenaline causes mydriasis due to contraction of radial muscles of iris(alpha 1)
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G.I.T Isolated gut prep… of animals on adr causes relaxation
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Bladder Dextrusor is relaxed (beta) and trigone (alpha)is constricted: both these actions results in hindrance of micturition
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Uterus Adr can both contract and relax uterine muscles respectively through (alpha) and (beta) receptors. HUMANS: contraction ..
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C.N.S Generally no effects ,but restlessness,apprehension,and tremor may occur . Activation of (alpha2) receptor in brain stem results in decreased sympathetic outflow -fall in bp-bradycardia
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Metabolic Glycogenolysis Hyperglycaemia Hyperlactacidaemia Lipolysis Inc …in ffa Calorigenesis
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Blood pressure Adr given by slow i.v infusion or s.c injection cause rise in systolic but fall in diastolic b.p peripheral resistance decreases because beta 2 receptors are more sensitive than alpha receptors .mean b.p increases .pulse pressure is increased . Rapid I . V injection of adr produces a marked increase in both systolic and diastolic b.p (at high conc in response alpha response predominates and vasoconstriction occurs even at skeletal muscles ).
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CAs not absorbed orally. Fate-Metabolism by MAO ( MAO-A in GIT wall) or COMT or both. ADME
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CVS- Palpitation tachycardia arrhythmias hypertension cerebral hemorrhage ADR’s Local necrosis gangrene CNS Anxiety fear nervousness tremors restlessness headache dizziness insomnia
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Therapeutic uses Cardiac resuscitation, Anaphylactic shock. Combined with local anesthetic to prolong its effect. It is used to control hemorrhage, in dental practice. In bronchial asthma
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