SYMPATHOMIMETIC AGENTS Flashcards
Catecholamines any compound
- hydroxyl is on_____carbon positions.
any compound that has CATHECOL nucleus (benzene ring with 2 adjacent hydroxyl groups with and amine containing side chain; 3,4
Endogenous catecholamines, 3
Epinephrine, norepinephrine, dopamine,
Sympathomimetic drugs does what?
mimic action of the SNS via activation of sympathetic receptors
Pharmacologic effects of catecholamines.
SV, HR, Force of contraction via receptor ______
Patients are more vulnerable to develop?
Cardiac stimulation (B1 receptors of heart)
- SV
- cardiac arrhythmias
Pharmacologic effects of catecholamines.
SVR, BP via receptor ______ mediated vaso________ of blood vessels
Shunts blood to ________(_______non essential organs)
Vasodilation results from _______activation in certain blood vessels such as _____ ______
Lung effect( Brandi/constri)
Inc/dec pulmonary blood flow.
GI effect on : secretions and motility
Cardiac stimulation (B1 receptors of heart)
-all increase
-constriction ; to muscle (vasoconstrict)
Alpha 1; skeletal muscle blood vessels.
bronchodilation
Improve pulmonary blood flow
Decreases GI motility and secretions
SYMPATHOMIMETIC
Increase nutritional supply
Modulation of the secretion of insulin, renin and pituitary hormones.
The predominant effect seen by the SNS for the ENDOCRINE SYSTEM
INHIBITION of INSULIN
Alteration that occur in the ANS in case of injury?
Effect in the eye? Enhancement of ______
Fluid retention
renin secretion –> angiontensin II –> Aldosterone
Posterior pituitary hormone secretion (ADH)
MYDRIASIS : far vision
They can alter potassium through?
Remember sodium potassium pump has ____receptors.
Beta 2 agonism by plasma epinephrine (Exogenously administered drug) produces HYPOKALEMIA, because Na -K pump has beta 2 receptors, which shift potassium from outside to the inside of the cell (RBCS and muscle cells)
CNS stimulation of Sympathomimetics?
is EPINEPHRINE a powerful CNS stimulant ?
Lipophillic enough drugs can cross brain
No; because it is a polar molecule
Analgesia : sympathomimetic with analgesia
enhanced specially in the presence of OPIOIDS
Physiological Basis of Adrenergic Receptor Function:
An important factor in the response of any cell, organ tissue to sympathomimetic agents is the _______ _________
density and proportion of ALPHA and BETA Adrenergic in various tissues.
For example: Norepinephrine as a drug does not activate
B2 receptor.
_________ and _________ can activate beta 2 receptors and are potent ________since they have affinity for _____receptors
Isoproterenol and epinephrine ; and Beta2 receptor.; BRONCHODILATORS; B2
NE and EPINEPHRINE cause vasoconstriction of _________ where as ISOPROTERENOL _______ effect on blood vessel. why? ______lacks
cause vasoconstriction of these blood vessels, where as ISOPROTERENOL HAS little effect on blood vessels since its lack alpha agonism activity
Explain the reflex homeostatic adjustments
The reflex homeostatic adjustments
Phenylephrine can cause ________ (side effect or adverse effect) (1)
Reflex BRADYCARDIA
Norepineprhine can cause activation of ______ reflex and ______ ____ tone leading to a ______ in HR.
Baroreceptor reflex
and increase VAGAL tone decreasing HR>
The most effective agents for enhancement of analgesia is ________ and __________
amphetamine and amphetamine derivatives
All sympathomimetic amines are derived by
beta phenylethylamine–> Benzene ring & Ethylamine side chain.
Basic catecholamines structure:
are monoamine substances with the presence of hydroxyl groups (-OH) specifically on the 3 and 4 carbon positions on the benzene ring
All sympathomimetic amines are derived by
beta phenylethylamine–> Benzene ring & EthylAMINE side chain.
_____makes polar and not lipid soluble. Catecholamines Catecholamines have a brief duration of action and are ineffective when administered orally because they are ?
Which 2 enzymes: _______ & ________
Hydroxyl group; rapidly inactivated in the intestinal mucosa and in the liver via both MAO & COMT before reaching the systemic circulation.
Sympathomimetic agents can exert their mechanism of action and pharmacologic effects by either _________ OR __________
DIRECTLY binding to and activating alpha-adrenergic, beta-adrenergic, or dopaminergic receptors
INDIRECTLY releasing substances which will bind to alpha-adrenergic, beta-adrenergic, or dopaminergic
receptors which activates the receptors