SNS

91問 • 1年前

問題一覧

What are the receptors of sympathetic

Alpha, Beta, Dopamine

It has the property of adjusting in response to stressful situations such as trauma, fear, hypoglycemia, cold or exercise.

Sympathetic nervous system.

The endogenous neurotransmitters contain three required structural features. What are those transmitter

Catechol nucleus, a,b- hydroxy group, Nitrogen substituents.

Ortho hydroxybenzene

Catechol 1& 2

Meta hydroxybenzene

Resorcino 1 & 3

Para hydroxybenzene

hydroquinone 1 & 4

The primary neurotransmitter of postganglionic sympathetic adrenergic nerves.

Norepinephrine.

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.

Receptors= Gq linked

Alpha 1

Receptors= Gi linked

Alpha 2

Exert negative feedback leading to decrease in the synthesis & release of NE

Alpha 2

(+) inotropism, dromotropism, chronotropism

Beta 1

The increase in cAMP levels in structures with beta2 receptors on them will lead to smooth muscle relaxation but skeletal muscle contraction.

Beta 2

modulation of motor activity, behavior, mood & thought process Induce vomiting

Dopamine 2-4

Gs linked

Dopamine 1

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

Receptors of catecholamines are example of

Type 2

Drugs that mimic the action of epinephrine or norepinephrine.

Adrenoceptor Agonists

What are under Nonselective

Epinephrine, Norepinephrine, Dopamine, Isoproterenol

What are under selective

ALPHA 1 agonists, ALPHA 2 agonists, BETA 1 agonists, BETA 2 agonists, DOPAMINE 1 agonists

Binds directly to the receptor

Direct acting.

Increase concentration of catecholamines in the synaptic cleft

Indirect acting.

CNS centered effects

Centrally acting

What are under increase release

Tyramine, Ephedrine, Angiotensin II, Amphetamine

What are under inhibit re uptake

TCAs, Cocaine, Reboxitine

What are under centrally acting

Phenylpropanolamine, Amphetamine, Methylphenidate, Phentermine, Modafinil

considered as the parent compound from which sympathomimetic drugs are derived.

Phenylethylamine.

consists of benzene ring with an ethylamine side chain

Phenylethylamine.

consists of benzene ring with an ethylamine side chain

Norepinephrine.

stimulates α1 , β1 and β2

Epinephrine

stimulates β1 and β2

Isoproterenol.

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.

Substitution of OH group on benzene ring increases maximal α & β activity

Benzene ring.

INACTIVATED BY COMT, cannot be given orally polar (Poor CNS penetration)

With OH (at 3 and 4) catecholamines

not inactivated by COMT, can be given orally, non polar (CNS penetration)

Without OH (at 3 and 4) non catecholamines

Dec. metabolism by monoamine oxidase (MAO).

Alpha carbon.

Give example of alpha carbon.

Ephedrine, Amphetamine

Substitution of OH group will become a direct-acting agonists. β-hydroxyl group.

Beta carbon.

Ephedrine, Phenylephrine and Amphetamine which of these are non catecholamines

All of them

Ephedrine, Phenylephrine and Amphetamine which of these are resistant to MAO metabolism

Amphetamine, Ephedrine

Ephedrine, Phenylephrine and Amphetamine which of these are direct acting agonist

Ephedrine, Phenylephrine

Ephedrine, Phenylephrine and Amphetamine which of these are direct acting agonist

Ephedrine, Phenylephrine

Ephedrine, Phenylephrine and Amphetamine which of these are indirect acting agonist

Amphetamine

What is the Natural catecholamines:

Epinephrine, Norepinephrine, Dopamine

What is the synthetic catecholamines:

Isoproterenol

OH groups show highest potency in activating alpha or beta receptors

High potency.

What are the rapid inactivation

COMT (POSTSYNAPTICALLY), gut wall, MAO (intraneurally), liver, gut wall

Catecholamines presence of OH group at 3 & 4 pos. OH group at this pos also inc. polarity

Inactivated by COMT

due to absence of substituent in alpha carbon

Inactivated by MAO

presence of OH at β carbon.

Direct acting agonist.

increase activity in beta receptors due to substituent in terminal amino group

Non selective

NE (Levophed)

Epi (adrenalin)

IV, SQ, Topical, Auto injector

Dopamine

Isoproterenol

IV, Inhalation

potent vasoconstrictor & cardiac stimulant. and Gives positive inotropic & chronotropic effect

Epinephrine.

Epinephrine (Adrenalin) Uses

Anaphylactic shock, bronchospasm, hypersensitivity, glaucoma

First line inotropic agent in the management of septic shock- (SBP <90mmHg) due to systemic infection

Norepinephrine

Norepinephrine also know as

Levarterenol, Noradrenaline

Norepinephrine (Levophed) Uses

Hypotension, Decongestant, infiltration anesthesia

immediate metabolic precursor of NE. Affinity to receptors:

Dopamine.

Dopamine uses

Septic shock, acute oliguric renal failure, Cardiogenic shock

Dec. activity in alpha receptor= bulky substituent in terminal amino group

Isoproternol

Isoproterenol uses

Asthma, COPD, Heart failure

What is the adverse effet oc Isoproterenol

Cardiac arrhythmias, Tachyphylaxis

What is the precursor of catecholamines

Tyrosine.

What ion is responsible for exit

Calcium ion

Dilation of pupil

Mydriasis.

What is the reponse to Alpha 1 receptors

Erection.

A receptor that has the ability to increase your blood pressure / Vasoconstriction

Alpha 1 receptors.

A type of blocker that has yhe ability to decrease your BP / Vasodilation

Alpha 1 blocker.

What alpha 1 Synthesis

Muscle contraction.

What do you call the space between pre synapse and post synapse

Synaptic cleft.

Decrease catecholamines secretion

NFE

What are the drugs that has NFE that decrease catecholamines secretion (norepinephrine and synthesis; Lowers blood pressure; Cure antihypertensive)

Clonidine, Methyldopa

Inotropic agent for heart failure

Beta 1 agonist

Increase the strength of cardiac contractions

Inotropic

Increase the duration of heart muscle that lead to heart failure

Chronotropism

Increase the conduct of cardiac cells

Dromotropism

A Catecholamines receptors that has an ability to increase heart rate and increase stroke volume.

Beta 1

A catecholamine receptors Juxtaglomerular cell if release its renin can increase blood pressure.

Beta 1

Facilitate the sodium and water retention in the body

Renin

A receptor that can decrease Blood pressure

Alpha 2

A catecholamines receptor that can increase Blood pressure

Beta 1

Used in mngt of bronchchi asthma and COPD

Beta 2

A catecholamines receptors that found in autonomic nervous system.

Dopamine 1

A catecholamines receptors that found in central nervous system.

Dopamine 2-4

High dopamine level can cause

Schizophrenia

Low dopamine level can cause

Parkinsonism

Anti parkinsonism

Dopamine 2 agonist

Antipsychotics drugs

Dopamine 2 antagonist

Cell structure.

Quinn Karylle Fuentes · 28問 · 2年前

Cell structure.