Adrenergic System Flashcards by Richhpal Singh

Sympathetic nervous system arises from

Thoracolumbar region

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Important Amino acid need for the formation of Noradrenaline in neuron

Tyrosine

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Rate limiting step in Noradrenaline synthesis

Conversion of Tyrosine to DOPA
Tyrosine hydroxylase - Rate limiting enzyme

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Drug that inhibits Tyrosine hydroxylase enzyme

Metyrosine

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VMAT-2 Receptors are present on

Present on Vesicles which is responsible for transportation of dopamine in vesicle

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Example of VMAT-2 Inhibitors

Reserpine
New drugs - Tetrabenazine
Deutetrabenazine
Valbenazine

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Drugs that inhibits entry of Noradrenaline in synapse

Guanethidine
Guanadrel

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Drugs that prevents reuptake of Noradrenaline

Cocaine - increases sympathetic activity

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Adrenergic receptors are classified into

Alpha receptors - Alpha-1 and Alpha-2
Beta receptors - Beta-1, Beta-2 and Beta-3

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Alpha-1 receptors acts on

Blood vessels - Vasoconstriction
Eye - Mydriasis
Prostatitic urthera - contracts (decreases urine outflow)

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Beta-1 receptors location and function

Heart - decreases HR (chronotropic), conduction (dromotropic) and Contractility (Inotropic)
JG cells of Kidney - Renin

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Beta-2 receptors location and function

Lungs - Bronchodilation
GIT - Constipation
Bladder - Relaxes bladder - decrease urine outflow
BV - Vasodilation
Uterus - relaxes uterus
Skeletal muscles - can cause tremors
Liver - glycogenolysis, gluconeogenesis

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Warning symptoms of Hypoglycemia

1) Tachycardia, Palpitations
2) tremors
3) Sweating

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Why beta blockers are contraindicated in diabetes patient

Can mask warning symptoms of Hypoglycemia
Also can block the reversal

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Sympathomimetic drugs can be divided into

Directly acting
Indirectly acting

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Location and function of Beta-3 receptors

Lipolysis
Bladder - relaxes bladder

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Beta-3 agonist used for overactive bladder

Mirabegron

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Indirectly acting Sympathomimetics

Cocaine
TCA
Ephedrine
Pseudoephedrine
Amphetamine

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Indirectly acting Sympathomimetics used as Nasal decongestants

Ephedrine
Pseudoephedrine

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Effects of Amphetamine

Decreases sleep
Increase attention span

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Amphetamine which is also termed as RAVE drug

Methylene dioxy methamphetamine

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DOC For Narcolepsy

Modafinil

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DOC for Attention deficit Hyperactivity Disorder (ADHD)

Methyl phenidate

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Catecholamines can be divided into

Endogenous - Adrenaline, Noradrenaline, Dopamine
Exogenous - Dobutamine, Fenoldopam, Isoprenaline

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Dopamine acts on which receptors

D1 - at low dose (<2mu/kg) - Vasodilation (max conc in Kidney) Beta 1 - at intermediate dose (2-10) Alpha-1 - at high dose (>10)

Uses of Dopamine

Acute CHF (2-10mu/kg) Shock (>10) DOC - if Shock+ Oliguria

Dobutamine acts on which receptors

Beta-1 receptors Used in Acute CHF

Fenoldopam acts on which receptors

Only acts on D1 receptors - Vasodilation Cam be indicated in Hypertensive emergency

Adrenaline, Noradrenaline and Isoprenaline acts on which receptors

Adrenaline - all receptors Nor adrenaline - alpha -1, alpha-2, Beta-1 Isoprenaline - Beta-1 , Beta-2

What is effect of Noradrenaline on Heart rate

Decreases

Which drug cause maximum pulse pressure

Isoprenaline

Adrenaline can be used in

DOC In Anaphylactic shock i.m, 1:1000 Im Cardiac arrest while giving CPR

What happened when alpha blocker given to patient with adrenaline producing tumor

Can result in vasomotor reversal of dale (Because of only beta -2 action)

Alpha-1 agonist used as eyedrop for Fundoscopy

Phenylephrine

Alpha-1 agonist drugs used in treatment of Hypotension

Methoxamine Mephentermine Midodrine

Alpha-1 agonist used as nasal decongestant

Oxymetazoline Xylomtazoline Naphazoline

Alpha -2 agonist drugs

Clonidine Methyldopa - used in treatment of Hypertension

Beta-2 agonist having tocolytic action

Ritodrine Isoxsuprine

Beta-2 agonist given as inhalational route

Salbutamol Salmeterol Formoterol Terbutaline

Alpha blockers can be divided into

Non selective alpha blocker Selective alpha-1 blocker Selective alpha-2 blocker - Yohimbine

Reversible non Selective alpha blockers are

Phentolamine Tolazoline Used in severe Hypertension Can cause tachycardia Short acting

DOC In Cheese reaction and Clonidie withdrawal

Phentolamine Tolazoline

Irreversible Non Selective alpha blocker

Phenoxybenzamine - used in Pheochromocytoma

Selective alpha blockers

'Zosin' Prazosin Terazosin Doxazosin Alfuzosin

Selective alpha blockers are used in

Mild to moderate hypertension Benign prostatic hyperplasia Peripheral vascular diseases Scorpion sting

Selective alpha-1A blocker drugs including

Tamsulosin Silodosin - not cause postural hypotension

Important side effect of Selective alpha -1 blockers

Orthostatic hypotension or Postural hypotension or First dose hypotension

Cardioselective beta blockers

New - Nebivolol Beta - Betaxolol Blockers - Bisoprolol Acts - Acebutolol Exclusively - Esmolol At - Atenolol Myo - Metoprolol Cardium - Celiprolol

Beta blockers having intrinsic sympathomimetic activity

Contain - Celiprolol Partial - Pindolol Agonistic - Alprenolol Activity - Acebutolol

Beta blockers having membrane stabilizing property

Black Na+ channels - local anesthetic property Possess - Propranolol Membrane stabilizing - Metoprolol Or Local - Labetalol Anaesthetic - Acebutolol Property - Pindolol

Water soluble Beta blockers

A - Atenolol N - Nadolol S - Sotalol

Longest acting beta blocker

Nadolol

Shortest acting beta blocker

Esmolol

Examples of third generation beta blockers

Any beta blockers that do Vasodilation (due to alpha blockade) Labetalol Carvedilol Nebivolol

Cardiac indications of Beta blockers

Hypertension MI Angina CHF Arrythmia HOCM

Extra cadiac indications of Beta blockers

Play - Performance anxiety The - Thyrotoxicosis G - Glaucoma A - Akathisia M - Migriane E - Essential tremors

Contraindications of beta blockers due to beta-1 blockade

Decreases HR - sick sinus syndrome Decreases conduction - AV blockade Decreases contractility - Acute CHF

Contraindications of Beta blockers due to beta-2 blockade

Diabetes Asthma Peripheral vascular disease Variant angina

Types of Glaucoma

Open angle glaucoma Closed angle glaucoma

Cause of Open angle glaucoma

Inreased production of aqeuous humor

Cause of closed angle glaucoma

Obstruction in drainage of aqeuous humor

Aqueous humor is drained from

Trabecular outflow Uveoscleral outflow

Drugs used to decrease formation of aqeuous humor

Alpha -1 agonist - vasoconstriction Beta blockers Carbonic anhydrase inhibitor

Alpha agonist used in glaucoma

Non selective alpha agonist - Adrenaline, Dipivefrine Alpha-2 agonist - Apraclonidine , Brimonidine

Beta blockers used in Glaucoma

Timolol Carteolol Levobunolol - longest acting Betaxolol Avoided in asthma patients

Carbonic anhydrase inhibitor used in Glaucoma

Acetazolamide oral or iv Brinzolamide Dorzolamide - locally eye drops

Drugs that increase trabecular outflow in glaucoma

Miotics - Cholinergic agonist - Pilocarpine Achesterase inhibitors - Physostigmine, Echothiophate

Side effects of Pilocarpine

Nasolacrimal duct stenosis

Side effects of Achesterase inhibitors

Cataract

Rho kinase inhibitors use in glaucoma

Netarsudil - acts by increasing outflow

Major side effect of Rho kinase inhibitors used in Glaucoma

Whorl like opacities in cornea/ Cornea verticillate

Drugs that increase uveoscleral outflow in glaucoma

Prostaglandins F2-alpha Latanoprost Bimatoprost Travoprost Tafluprost

Adverse effects of Miotics

Nasolacrimal duct stenosis Cataract Retinal detachment

Side effects of Beta blockers in Glaucoma

A - Asthma precipitates B - Block - AV block C - Acute CHF D - Diabetes

Side effects of PGF2-Alpha

Fluid in macula(macular edema) Pigmentation of iris (Heterochromia iridis) Growth of eyelashes (Hypertrichosis)

Side effect of Apraclonidine

Lid retraction

Side effects of Brimonidine

Brain suppression - contraindicated in infants less than 2 years

Side effect of Adrenaline in Glaucoma

Adrenochrome - Conjunctival pigmentation