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Catecholamines (4)
- Epi
- NE
- Isoproterenol
- Dopamine
- (ENID, OK)
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Epi does what to receptors specifically on vessels
- Stimulates all Alpha and Beta receptors
- Stimulates Alpha (vasocostriction) and Beta (vasodilation) = (there are less B2 than A, but B2 are more sensitive to Epi. (small amt=B2) (large bolus=A) (medium=pressor than depressor)
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Epi on heart
Stimulate B1 to increase HR and contractility
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Epi on metabolism
Stimulate Betas to increase glucose in blood in all possible ways (Gluconeo, gycogen break down and none formed, fats to fatty acids)
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Epinephrine (duration and administration and for what?)
- Start duration, not given orally, given by inhalation or parenterally
- Treats asthma and bronchiospasms of anaphylactic shock
- Stimulate Betas to increase glucose in blood in all possible ways (Gluconeo, gycogen break down and none formed, fats to fatty acids)
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is a chemical classification of amine molecules containing a benzene ring with OH substitutions at the 3 and 4 positions.
catecholamine
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2 catecholamines that act as neurotransmitters in the CNS
Dopamine and Epinephrine
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Tyrosine -->
_____ -->
Dopamine --->
______
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rate limiting step in conversion of tyrosine to Norepinephrine
Tyrosine to DOPA
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reason catecholamines aren't effective when given orally
enzymes MAO and COMT readily break them down in liver
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mechanism for the termination of NE action where NE is taken back into the presynaptic terminal
uptake I (most important 60-90% of the time)
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Some NE enters the post synaptic cell where it is enzymatically inactivated by the extra-neuronal enzyme, catechol-O-methyltransferase (COMT).
uptake II
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is found in nerve terminal (mitochondrial membrane) and is in very high concentration in the liver.
MAO
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is found in the effector cells and in high concentration in the cytosol of the liver cells.
COMT
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mimic sympathetic function. They can do this either by directly stimulating the adrenergic receptors, or indirectly, by allowing more norepinephrine to be present in the synaptic cleft. Indirect acting _____ either cause release of the transmitter (NE) or prevent the normal termination of action (reuptake).
Sympathomimetic drugs
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Endogenous sympathetic substances not effective when given orally
catecholimines
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Norepinephrine (3)
- Acts on all As and Bs
- Increases BP by stimulating As on Blood vessels (vasoconstriction and increased CO)
- Not clinically useful b/c short duration, not orally effective
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Isoproterenol
- Beta stimulatn only
- produces bronchodilation (B2)
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Dopamine
- metabolic precursor of Epi and NE
- Used for Parkinson's (L-Dopa), is used as neurotransmitter in CNS
- Treat compromised renal blood flow
- High dose=stimulate A and B receptors --> increases BP and HR
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non-catecholamine Alpha Agonists (6)
- Tyramine
- Amphetamine
- Methylphenidale (Ritalin)
- Ephidrine
- Phenylephrine
- Methaxomine
- (you can't TAME shelly in the PM, these also excite most thing so that works)
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non-catecholamine Alpha Agonists that are nasal decongestants
- Ephidrine
- Phenylephrine
- Methaxomine
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Cause massive release of NE ---> Increases BP
Inactivated by MAO
Needs NE in neuron for results (false transmitter)
Alpha Agonist
Tyramine
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Indirect actions
orally effective
enter CNS
Toxic can be lethal
Cerbral hemorrhage due to vasoconstriction
can readily diffuse into the nerve terminal to cause NE release
Use in hyperkinetic kids and narcoleptics
Alpha Agonist
Amphetamine and Methamphetamine
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Indirect action
use for ADHD
oral use
addictive
CNS escilation
Methylphenidale (Ritalin
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direct and indirect actions
Acts on all A and Bs directly
Causes bronchodilation (decongestion)
short lasting mydriasis (dilation)
Ephedrine
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Direct action
produce mydriasis
only orally effective in huge doses
rebound effect in nasal congestant
Phenylephrine
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Direct action
causes mydriasis
atrial tachycardia treatment
nasal decongestant
Methaxomine
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Beta agonists (6)
- Salmeterol
- Metaproterenol
- Albuterol
- Rifrodine
- Terbutaline
- Dobutamine
- (SMART D, that's me I'm also B+ blood type so it works)
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Direct-Beta2 selectivity
Bronchial asthma
cardiac side effects
Metaproterenol
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Direct Beta 2 selection
long duration than metaproterenol
bronchodilator
prevent premature labor
Terbutaline
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Direct Beta 2
Asthma
Salmeterol
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Direct Beta 2
relax uterus
delay premature labor FDA approved
Rifrodine
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Direct Beta 2
Increase Cardiac Output w/ out vasoconstriction
Cardiac insufficiency, CHF
cardiac surgery
rapidly metabolized by liver
does not stimulate dopamine receptors
Dobutamine
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Reuptake blockers
- Cocaine
- Tricyclic Anti-depressants
- (CT scan?)
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Blocks reuptake 1
NE reuptake
Cocaine
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Catecholamine reuptake
Tricyclic Anti-depressants
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Blockers of Adrenergic Nerves
- Clonidine
- Alpha-Methyl Dopa
- Alpha-Methyl-Paratyrosine
- (BAN CAMP AMD)
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Blockers of Adrenergic Nerves MAOs (7)
- a) depression of CNS sympathetic tone
- b) inhibition of NE synthesis
- c) false transmitter production
- d) deplation of catecholamine storage
- e) prevention of action potential effectiveness
- f) destruction of adrenergic nerve terminals
- g) ganglionic and receptor blockade
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Drugs that are taken up by pump that takes in NE shouldn't be administered with what drugs for what reason.
reuptake inhibitors b/c they will prevent their action b/c they aren't being transported
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Antihypertensive
Alpha 2 stimulant in CNS -->decreases sympathetic tone to blood vessels and heart
EtOH and opiod addiction helper
Synergestic effect w/opiods
Clonidine
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Decrease BP Decrease sympathetic tone
Alpha 2 agonists
Not metabolized by MAO
CNS
Alpha-Methyl Dopa
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Drugs that stimulate Alpha 2 produce what in BP.
- vasoconstriction in periphery but hypotensive action in CNS for hours.
- This is called CNS acting sympatho-inhibitory agents
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Decreases NE in postganglion b/c it is a substrate for tyrosine hydroxylase which is the rate-limiting step in NE formation
Alpha-methyl-para tyrosine
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Agents that are taken up by adrenergic neurons, metabolized to an active amine, stored with NE in vesicles and released with NE by an action potential are called false transmitter precursors.
false transmitter precursor
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Several drugs act to deplete catecholamines from sympathetic nerve endings and thus reduce sympathetic reactivity.
Catecholamine depletion
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Catecholamine depletion
- Reserpine
- Guanethidine
- 6-OH Dopa
- (RG-6 on a CD)
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interrupts storage of NE, Epi, Dopa in vesicles
decreases BP redirectly
Enters CNS
Reserpine
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Deplete NE - blocks AP
Potent antihypertensive drug
no pass BBB
Guanethidine
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destroys nerve terminals
6-OH Dopa
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Alpha Blockers
- Phentolamine
- Phenoxybenzamine
- Prazosin
- Terazosin/Doxazosin
- Yohimbine
- Clonidine and Alpha-Methyldopa
- (I got nothing to help)
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Alpha 1 preference
short action
Phentolamine
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Alpha 1 preference
Long duration
Can become irreversible (competitive --> non-comp inhibition)
Phenoxybenzamine
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Alpha 1 selection
No large tachycardia reflex
decrease BP
Prazosin
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Like Prazosin
Treat benign hypertrophic prostates
Terazosin/Doxazosin
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select Alpha 2
prevents effects of hypotensive dopamine
Yohimbine
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Experimental studies in pts w/spinal cord damage show Alpha blockage in these drugs (2)
Clonidine and methyldopa
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Beta Blockers
- Piadolol
- Propranolol
- Alenolol
- Metaprolol
- Betarolol
- Esmolol
- Nadolol
- Timolol
- (PPAM BENT)
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Beta 1 & 2 blockage
Decrease BP
Propranolol
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Beta 1 selective
Decrease Plasma Renin
Metaprolol
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Beta 1 selective
less CNS side effects than Metaprolol
Excrete by kidneys
Alenolol
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Nonselective
Intrinsic Sympothemimetic Activity --> stimulate Beta 1 (tolerated better during exercise)
Piadolol
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Potent Beta 1 & 2 Blocker
Treat open angle glaucoma
Prevent reinfections to myocardium
Decrease intraoccular pressure
Timolol
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Non-selective
long duration
Nadolol
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Beta 1 selection
Liver metabolism
Long 1/2 life
Betarolol
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Beta 1 selection
short 1/2 life
Control ventricular HR for emergency or critically ill
Esmolol
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Alpha and Beta Blockers
- Labetalol
- Carvedilol
- (LC blocked heidi and spencer)
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Beta 1&2 and alpha blocker
blockage toward Alpha 2
Some Beta 2 - stimulation
lower plasma Renin
lower BP
small reflex effect on HR or CO
Labetalol
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Similar actions to labetalol
"Free Radical Scavenger"
Protects heart cells from damage
Approved for pts w/congestive heart failure
Carvedilol
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