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Adrenergic Agonists

Drug Action Receptor Therapeutic Uses Pharmacokinetics Adverse Effects Other


Epinephrine -at low doses, β effects on the vascular α and β -DOC in: acute -rapid onset, but -CNS: anxiety, -catecholamine
(Direct) system (vasodilatation) asthma, brief duration of fear, tension, -synthesized from dopamine in
-at high doses, α effects are stronger anaphylactic shock action headache, tremor the adrenal medulla
(vasoconstriction) -Open-angle -can be given IV, -Cerebral -metabolized by COMT and
-Strengthens the contractility of the glaucoma (2% soln SC, endotracheal hemorrhage MAO; final metabolites in urine
myocardium and increases the rate of topically) tube, inhalation, -Cardiac are metanephrine,
contraction (β1) -Restore cardiac topically to eye arrhythmias, vanillylmandelic acid
-constricts arterioles in the skin, mucous rhythm in patients particularly in -rather than epinephrine, β2
membranes and viscera (α effects) with cardiac arrest patients on agonists like ALBUTEROL are
-dilates BV to liver and skeletal muscle -Used in digitalis favoured in chronic Tx of asthma
(β2) combination with -Pulmonary -enhanced CV action in pts with
-Increase in systolic pressure, decrease local anesthetics to edema hyperthyroidism
in diastolic pressure increase the -exaggerated CV response in
-Bronchodilation (β2) duration of the presence of cocaine
-Inhibits the release of allergy anesthesia -in diabetics, if epi is being used,
mediators -Weak solutions insulin may have to be increased
-Increased glycogenolysis in the liver, can be used -β-blockers block effect of β-
increased release of glucagon (β2 topically to control receptors, leaving α-receptors
effect) oozing of capillary unopposed (increase in BP)
-decreased release of insulin (α2 effect) blood -inhalation anesthetics sensitize
-initiates lipolysis (β receptors) the heart to effects of
epinephrine
Norepinephrine/ -vasoconstriction of most vascular beds α- -Shock -IV -Similar to -catecholamine
Levarterenol causing rise in peripheral resistance receptors -Duration of action epinephrine -METARAMINOL preferred over
(Direct) -systolic and diastolic pressure increases 1-2 minutes at the -Blanching and NE for shock because it doesn’t
-if ATROPINE blocks transmission of end of the infusion sloughing of skin reduce blood flow to kidneys like
vagal effects before giving NE, period along injected NE
stimulation of heart causes tachycardia -poorly absorbed vein
-increased force of contraction in the with SC injection
heart (+ve ionotropic effect)
Isoproterenol -increases rate and force of contraction β1 and β2 -AV block -Sublingual -similar to -synthetic catecholamine
(Direct) of the heart receptors -Cardiac arrest -Parenterally epinephrine -stable to MAO, minor substrate
-Dilates arterioles of skeletal muscle, -Acute asthma -Inhaled aerosol for COMT
resulting in decreased peripheral attack (inhalation)
resistance (β2 effect)
-slight increase in systolic pressure, but
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Adrenergic Agonists

great reduction in mean arterial and


diastolic pressure
-profound and rapid bronchodilation
Dopamine -at lower doses it stimulates β1 cardiac α, β, D1, -DOC for shock -same effects as -catecholamine
(Direct) receptors (inotropic and chronotropic) D2 (continuous sympathetic -found in CNS basal ganglia and
-at higher doses it causes vaso- infusion) stimulation adrenal medulla
constriction by activating α1 receptors -rapidly metabolized by MAO or
-D1 and D2 activation produces COMT to homovanillic acid,
vasodilatation of peripheral mesenteric therefore adverse effects are
and renal vascular beds short-lived
-D2 receptors found on presynaptic
adrenergic neurons interfere with
release of NE when activated
Dobutamine -increases cardiac rate and output β1 -increase CO in CHF -increases AV -synthetic catecholamine
(Direct) -inotropic support conduction, so -available as a racemic mixture
after cardiac cautious use in (optically inactive)
surgery atrial fibrillation -increases the CO, with little
-tolerance may change in HR, and doesn’t
develop on increase O2 demand of
prolonged use myocardium significantly
Oxymetazoline -used locally in the eye or nose as a α1 and α2 -ophthalmic drops -available as nasal -Nervousness -synthetic
(Direct) vasoconstrictor for redness of eyes spray -Headaches -absorbed into systemic
-direct stimulation of α receptors on BV associated with -Trouble sleeping circulation regardless of route of
supplying nasal mucosa and conjunctiva swimming, colds, -Rebound administration
to reduce blood flow and decrease contact lenses congestion w/
congestion long term use
Phenylephrine -vasoconstrictor that raises systolic and Favours -Mydriasis -Hypertensive -synthetic drug
(Direct) diastolic pressures α1 (ophthalmic headache -not a substrate for COMT
-induces reflex bradycardia when given receptors solution) -Cardiac
parenterally over α2 -Raise BP irregularities
-acts as a nasal decongestant and -Terminate
produces prolonged vasoconstriction episodes of
supraventricular
tachycardia
Methoxamine -raises BP by stimulating α1 receptors in Favours -Attacks of -Hypertensive - synthetic drug
(Direct) the arterioles, causing vasoconstriction α1 paroxysmal headache -does not tend to trigger cardiac

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Adrenergic Agonists

receptors supraventricular -Vomiting arrhythmias in the heart


over α2 tachycardia
-To overcome
hypotension during
surgery involving
halothane
anesthetics
Clonidine -acts centrally to produce inhibition of α2 -In essential HTN,
(Direct) sympathetic vasomotor centre, to lower BP
decreasing sympathetic outflow to the -Minimize
periphery symptoms due to
withdrawal from
opiates or
benzodiazepines
Metaproterenol -produces dilation of the bronchioles β2 > β1 -Asthma -orally or inhalation -chemically similar to
(Direct) and improves airway function -Reverse ISOPROTERENOL
bronchospasm -resistant to methylation by
COMT
Albuterol β2 -Bronchodilator -short-acting -produce equal bronchodilation
Pirbuterol -administered by with less cardiac stimulation
Terbutaline metered-dose
(Direct) inhaler
Salmeterol β2 -Bronchodilator -single dose by -selective, long-acting
Formoterol -DOC treating metered-dose -Salmeterol has somewhat
(Direct) nocturnal asthma inhalation device delayed onset of action
in symptomatic pts provides -highly efficacious when
taking other bronchodilation combined with a corticosteroid
asthma medication over 12 hours
Amphetamine -central stimulatory action α, β, CNS -Hyperactivity in -use in pregnancy should be
(Indirect) -increases blood pressure by α- children avoided due to adverse effects
stimulatory action on vasculature and β- -Narcolepsy on developing fetus
effects on the heart -Appetite control
-peripheral actions are mediated
through blockade of NE uptake and
cellular release of stored
catecholamines

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Adrenergic Agonists

Tyramine -can enter nerve terminals and displace -not clinically -found in fermented foods (ripe
(Indirect) stored NE useful cheese, Chianti wine)
-released catecholamines act of -normal byproduct of tyrosine
adrenoceptors metabolism
-oxidized by MAO in GIT, but if
patient is on MAO inhibitors, it
can cause vasopressor episodes
Cocaine -blocks the Na+/K+ ATPase which is α, β -pts taking cocaine have greater
(Indirect) required for uptake of NE effects produced by small doses
-increases blood pressure by α- of catecholamines and longer
stimulatory action on vasculature and β- duration of action
effects on the heart

Ephedrine -release stored NE and also directly α, β, CNS -Ephedrine: -Long duration of -plant alkaloids, now made
Pseudo- stimulate the receptors prophylactic in action synthetically
ephedrine -penetrate into CNS, but pseudo has chronic treatment -Excellent -poor substrates for COMT and
(Mixed-action) less CNS effects of asthma absorption orally MAO
-Ephedrine raises systolic and diastolic -Ephedrine: -Ephedrine -Pseudo has been illegally
pressures by vasoconstriction and enhances eliminated in urine, converted into
cardiac stimulation contractility and unchanged methamphetamine
-Ephedrine produces bronchodilation, motor function in -Pseudo partially
more slowly and less potency than EPI myasthenia gravis metabolized in
or ISOPROTERENOL -Ephedrine: raise liver, then
-Ephedrine causes stimulation of CNS BP eliminated in urine
resulting in increased alertness, -Pseudo: nasal and
decreased fatigue, prevents sleep, sinus congestion or
improved athletic performance congestion of
Eustachian tubes

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