問題一覧
1
What are the receptors of sympathetic
Alpha , Beta, Dopamine
2
It has the property of adjusting in response to stressful situations such as trauma, fear, hypoglycemia, cold or exercise.
Sympathetic nervous system.
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The endogenous neurotransmitters contain three required structural features. What are those transmitter
Catechol nucleus, a,b- hydroxy group , Nitrogen substituents.
4
Ortho hydroxybenzene
Catechol 1& 2
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Meta hydroxybenzene
Resorcino 1 & 3
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Para hydroxybenzene
hydroquinone 1 & 4
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The primary neurotransmitter of postganglionic sympathetic adrenergic nerves.
Norepinephrine.
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Synthesized inside nerve axon in the adrenal medulla and stored within vesicles. It is released by the nerve when an action potential travels down the nerve.
Norepinephrine.
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Receptors= Gq linked
Alpha 1
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Receptors= Gi linked
Alpha 2
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Exert negative feedback leading to decrease in the synthesis & release of NE
Alpha 2
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(+) inotropism, dromotropism, chronotropism
Beta 1
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The increase in cAMP levels in structures with beta2 receptors on them will lead to smooth muscle relaxation but skeletal muscle contraction.
Beta 2
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modulation of motor activity, behavior, mood & thought process Induce vomiting
Dopamine 2-4
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Gs linked
Dopamine 1
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like family receptors is coupled to the G protein Gi, which directly inhibits the formation of cAMP by inhibiting the enzyme adenylate cyclase
Dopamine 2-4
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Receptors of catecholamines are example of
Type 2
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Drugs that mimic the action of epinephrine or norepinephrine.
Adrenoceptor Agonists
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What are under Nonselective
Epinephrine, Norepinephrine, Dopamine, Isoproterenol
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What are under selective
ALPHA 1 agonists , ALPHA 2 agonists , BETA 1 agonists , BETA 2 agonists , DOPAMINE 1 agonists
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Binds directly to the receptor
Direct acting.
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Increase concentration of catecholamines in the synaptic cleft
Indirect acting.
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CNS centered effects
Centrally acting
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What are under increase release
Tyramine, Ephedrine, Angiotensin II , Amphetamine
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What are under inhibit re uptake
TCAs, Cocaine, Reboxitine
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What are under centrally acting
Phenylpropanolamine , Amphetamine, Methylphenidate, Phentermine, Modafinil
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considered as the parent compound from which sympathomimetic drugs are derived.
Phenylethylamine.
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consists of benzene ring with an ethylamine side chain
Phenylethylamine.
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consists of benzene ring with an ethylamine side chain
Norepinephrine.
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stimulates α1 , β1 and β2
Epinephrine
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stimulates β1 and β2
Isoproterenol.
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Methyl substitution on NE, yielding Epi, enhances activity at β2 receptors. ↑ β-receptor activity. The larger the substituent on the amino group, the lower the activity at α-receptor.
Terminal amino group.
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Substitution of OH group on benzene ring increases maximal α & β activity
Benzene ring.
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INACTIVATED BY COMT, cannot be given orally polar (Poor CNS penetration)
With OH (at 3 and 4) catecholamines
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not inactivated by COMT, can be given orally, non polar (CNS penetration)
Without OH (at 3 and 4) non catecholamines
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Dec. metabolism by monoamine oxidase (MAO).
Alpha carbon.
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Give example of alpha carbon.
Ephedrine , Amphetamine
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Substitution of OH group will become a direct-acting agonists. β-hydroxyl group.
Beta carbon.
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Ephedrine, Phenylephrine and Amphetamine which of these are non catecholamines
All of them
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Ephedrine, Phenylephrine and Amphetamine which of these are resistant to MAO metabolism
Amphetamine, Ephedrine
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Ephedrine, Phenylephrine and Amphetamine which of these are direct acting agonist
Ephedrine, Phenylephrine
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Ephedrine, Phenylephrine and Amphetamine which of these are direct acting agonist
Ephedrine, Phenylephrine
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Ephedrine, Phenylephrine and Amphetamine which of these are indirect acting agonist
Amphetamine
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What is the Natural catecholamines:
Epinephrine, Norepinephrine, Dopamine
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What is the synthetic catecholamines:
Isoproterenol
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OH groups show highest potency in activating alpha or beta receptors
High potency.
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What are the rapid inactivation
COMT (POSTSYNAPTICALLY), gut wall , MAO (intraneurally), liver, gut wall
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Catecholamines presence of OH group at 3 & 4 pos. OH group at this pos also inc. polarity
Inactivated by COMT
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due to absence of substituent in alpha carbon
Inactivated by MAO
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presence of OH at β carbon.
Direct acting agonist.
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increase activity in beta receptors due to substituent in terminal amino group
Non selective
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NE (Levophed)
IV
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Epi (adrenalin)
IV, SQ, Topical, Auto injector
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Dopamine
IV
55
Isoproterenol
IV, Inhalation
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potent vasoconstrictor & cardiac stimulant. and Gives positive inotropic & chronotropic effect
Epinephrine.
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Epinephrine (Adrenalin) Uses
Anaphylactic shock , bronchospasm, hypersensitivity, glaucoma
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First line inotropic agent in the management of septic shock- (SBP <90mmHg) due to systemic infection
Norepinephrine
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Norepinephrine also know as
Levarterenol, Noradrenaline
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Norepinephrine (Levophed) Uses
Hypotension , Decongestant , infiltration anesthesia
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immediate metabolic precursor of NE. Affinity to receptors:
Dopamine.
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Dopamine uses
Septic shock , acute oliguric renal failure, Cardiogenic shock
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Dec. activity in alpha receptor= bulky substituent in terminal amino group
Isoproternol
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Isoproterenol uses
Asthma, COPD, Heart failure
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What is the adverse effet oc Isoproterenol
Cardiac arrhythmias , Tachyphylaxis
66
What is the precursor of catecholamines
Tyrosine.
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What ion is responsible for exit
Calcium ion
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Dilation of pupil
Mydriasis.
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What is the reponse to Alpha 1 receptors
Erection.
70
A receptor that has the ability to increase your blood pressure / Vasoconstriction
Alpha 1 receptors.
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A type of blocker that has yhe ability to decrease your BP / Vasodilation
Alpha 1 blocker.
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What alpha 1 Synthesis
Muscle contraction.
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What do you call the space between pre synapse and post synapse
Synaptic cleft.
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Decrease catecholamines secretion
NFE
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What are the drugs that has NFE that decrease catecholamines secretion (norepinephrine and synthesis; Lowers blood pressure; Cure antihypertensive)
Clonidine, Methyldopa
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Inotropic agent for heart failure
Beta 1 agonist
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Increase the strength of cardiac contractions
Inotropic
78
Increase the duration of heart muscle that lead to heart failure
Chronotropism
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Increase the conduct of cardiac cells
Dromotropism
80
A Catecholamines receptors that has an ability to increase heart rate and increase stroke volume.
Beta 1
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A catecholamine receptors Juxtaglomerular cell if release its renin can increase blood pressure.
Beta 1
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Facilitate the sodium and water retention in the body
Renin
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A receptor that can decrease Blood pressure
Alpha 2
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A catecholamines receptor that can increase Blood pressure
Beta 1
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Used in mngt of bronchchi asthma and COPD
Beta 2
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A catecholamines receptors that found in autonomic nervous system.
Dopamine 1
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A catecholamines receptors that found in central nervous system.
Dopamine 2-4
88
High dopamine level can cause
Schizophrenia
89
Low dopamine level can cause
Parkinsonism
90
Anti parkinsonism
Dopamine 2 agonist
91
Antipsychotics drugs
Dopamine 2 antagonist