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79 Cards in this Set

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Sympathetic receptors important to note:
B1 - in heart, increase CO
A1 - contraction in peripheral arterioles
B2 - bronchial smooth muscle, certain GI, and in blood vessels supply skeletal muscles
What does the adrenal medulla predominately secrete?
MOSTLY epinephrine (2/3)
1/3 norepinephrine
Describe synthesis of NE?
Tyrosine converted to L-dopa by tyrosine hydroxylase (RLS)
Major ways to terminate NE signal?
Major way - NE transporter, uptake 1
Extraneuronal transporter - uptake 2
Alpha 2 receptors (negative feedback, inhibit NE release)
Drugs that decrease NE transmission:
a-methyltyrosine
carbidopa, a-methyldopa
disulfiram
reserpine
guanethidine
receptor antagonist
Drugs that increase NE transmission:
Amphetamine, tyramine
Cocaine
Receptor agonist
alpha-methyl tyrosine
MOA: inhibit tyrosine hydroxylase, affecting NE synthesis
Uses: pheocromocytoma
ASE: hypotension, sedation
Reserpine
MOA: affects NE release by depleting NE stores via VMAT inhibition
Uses: hypertension (obsolete)
ASE: same as methyldopa, depression, parkinson disorders
Imipramine
Drug affecting NE uptake by blocking neuronal transport.
Uses: Depression
ASE: atropine like side effects, arrhytmias
Guanethidine
MOA: affects NE release, neuronal damages
Uses: hypertension (obsolete)
ASE: same as methyldopa, initial increase in BP
Cocaine
MOA: blocks NET
Uses: drug abuse
ASE: hypertension, excitement, convulsion
Methyldopa
MOA: false transmitter precursor to inhibit NE synthesis
Uses: hypertension in pregnancy
ASE: hypotension, drowsiness, diarrhea impotence
Carbidopa
MOA: inhibits DOPA decarboxylase, affecting NE syntehsis
Uses: adjunct to LDOPA for peripheral effects. Whatever
Where do you find a1 receptors, and what do they do?
VSM - contraction (IP3/DAG)
Pupillary dilator muscle -Contraction (dilates pupil)
Pilomotor smooth muscle - erects hair
What do you find a2 receptors and what do they do?
Postsynaptic CNS adrenoceptors - decrease cAMP
Platelets - aggregation (decrease cAMP)
Adrenergic/cholinergic nerve terminals - inhibition of trasmitter release
Some VSM - Decrease cAMP and decrease contraction?
Fat cells - inhibition of lipolysis, decrease cAMP
Where do you find B1 receptors and what do they do?
Heart, fat cells, glomerular cells - activate adenylate cyclase
Where do you find B2 receptors and what do they do?
respiratory, uterine, and VSM - activate adenylate cyclase
Where do you find B3 receptors, what do they do?
Fat cels - activates lipolysis
Where do you find B4 cells, what do they do?
CNS - involved in long term memory
Where do you find D1 receptors?
smooth muscle - dilates renal blood vessels
Where do you find D2 receptors?
CNS nerve endings - modulates transmitter release
Dobutamine
B1 agonist
Methoxamine
a1/a2 agonist
Phenylephrine
a1/a2 agonist
Isoproterenol
b1/b2 agonist
Epinephrine
a1/a2/b1/b2 agonist
Norepinephrine
a1/a2/b1 agonist
What isomers of beta blockers actually work?
S (L) isomer.
What as the differences in isomers of Propanolol?
L isomer - has B blocking action
D isomers - doesn't, but still has local anesthetic function
What drugs are not susceptible to MAO?
Isoproternol (b/c if has big substitution group, though it can be oxidized by COMT)
Amphetamine - not susceptible to MAO OR COMT, and can cross BBB b/c it doesn't have hydroxyl group. Yikes. abused
What are the indirect acting sympathomimetics (that act by increase NE)?
Amphetamine
Methamphetamine
Tyramine
Phenylpropranolamine
Ephedrine (and pseudoephedrine)
Amphetamine uses/ASE
Use: narcolepsy, ADD, suppress appetite (no longer used)
ASE: restlessness, dizziness, insomnia, impotence, cardiac arrhythmias, hypertensive crisis with MAO inhibitors
Ephedrine (pseudoephedrine)
Use: vasoconstriciton, bronchodilation
ASE: hypertension, insomnia, tachyphylaxis
Tyramine
Present in wines, beer, cheese, no relevant clinical uses
ASE: incombo with MAO inhibitors could lead to sympathetic crisis and be potentially fatal
Remember the qiss and qiq till your siq of sqs analogy:
a1a2b1b2
m1m2m3
d1d2h1
h2v1v2
What sympathetic receptors mediate lipolysis?
B1
What receptors on skeletal muscle cells can, when stimulated, uptake K and lead to hypokalemia?
B2
What two drugs were used in the lecture to test the baroreceptor reflex (ie they increase/decrease bp)?
Phenylephrine - vasoconstriction and increase BP (increase PARA)
Histamine - vasodilation and decrease BP (increase SYMP)
What receptors control peripheral resistance?
a1 vasoconstricts
b2 vasodilates
What receptors modulate blood pressure?
systolic - b1 HR
diastolic - a1 TPR
If you stimulate a1, a2, and b1 receptors together with norepi, what will happen to HR, BP, and TPR?
BP will increase
HR will DECREASE (despite stimulating B1, because the baroreceptors reflex is also active due to increase BP. The B1 stimulation DOES cause increase contractility and CO, therfore systolic pressure INCREASES. I know this isn't intuitive
TPR also goes up and causes the BP to go up, you get this.
If you stimulates a1, a2, b1, b2 receptors together with epi, what will happen to HR, BP?
HIGH DOES - it acts JUST the same as NE (raises BP, TPR, and lowers HR)
BUT
LOW DOSE - accentuates action of B2 receptors (which vasodilate) - diastolic pressure goes down, systolic goes up
If you stimulates JUST B receptors with isoproterenol, what will that do?
It will dramatically decrease TPR (stimulating B2, and there is no more alpha action, only B2 relaxing)
AND
decrease in diasotlic BP, slight increase in systolic BP (BP goes down overall b/c of the combo effect of both B recepors)
HR will go up in response to low BP and B1 stimulation
What do the 2 dopamine receptors do?
D1 - mostly in BV, increase cAMP and cause vasorelaxation at lo doses and B1 activation at higher, a1 at high high doses
D2 - CNS, cause hypotension, decrease HR
Dopaminergic receptor antagonist mentioned
Haloperidol (used in low doses as renal vascular dilator, and medium doses to increase cardiac contraction), HIGH doses to increase vasconsriction (a1 recetors)
What receptors are most sensitive to the drugs epi, norepi, and isop?
A1 - Epi > NE >> Iso
A2 - Epi > NE >> Iso
B1 - Isop > Epi = NE
B2 - Isop > Epi >> NE
A1 agonist
Phenylephrine
Midodrine
A2 agonist
Clonidine
Dexmedetomidine
A1 antagonist
Prazosin
Terazosin
Phentolamine
A2 antagonist
Yohimbine
Tolazoline
Phentolamine
B1 agonist
Dobutamine
B1 antagonist
Metoprolol
Atenolol
Propranolol
B2 agonist
Terbutaline
Albuterol
B2 antagonist
Propranolol
Butoxamine
Phenylephrine (neosynephrine)
Alpha 1 agonist
Nasal decongestant, mydriatic agent (pupil dilation), vasconstriction to localize local anesthetic
ASE: Hypertension, headache, tissue necrosis
Metaraminol
alpha 1 agonist
both direction acting and releases NE (mixed acting). Treats hypotension, off-label use to relieve paroxysmal tachycardia
Midodrine (prodrug)
alpha 1 agonist
treats Orthostatic hypotension, chronic fatigue syndrome
ASE: supine hypertension, piloerection, urinary retention.
Clonidine
a2 receptor agonist, passes BBB and activates a2 in medulla, decrease sympathetic outflow to heart. Does NOT interfere with baroreceptor function, does NOT product postural hypotension
used: hypertension, opiate and benzodiazepine withdrawal
ASE: Xerostomia (dry mouth), sedation, constipation, sexual dysfunction
Dexmedetomidine
a2 agonist used as sedative during VN surgery
Dobutamine
Selective B1 agonist
Positive inotropy with less increase in HR.
It's short term treatment of cardiac decomp with little change in myocardial O2 demand. Can desensitize D receptors.
ASE: tachyarrhythmias, angina, hypertension
B2 agonist mentioned, and how they funciton
Terbutaline
Albuterol
Ritodrine
Treat bronchospasms/asthma, delays premature labor.
ASE: nausea, vomiting, tachycardia, palpitations, termors, hypertension.
Phenoxybenzmine
Irreversible alpha antagonist
Used: peripheral vascular disease and control complications associated with excessive (pheochromocytoma)
ASE: tacycardia, postural hypotension, miosis, nasal stuffiness, failure of ejaculations
Phentolamine
Reversible alpha antagonist
Use: peripheral vascular disease, pheochromocytoma treatment
ASE: tachycardia, postural hypotension, miosis, nasal stuffiness
Prazosin
Selective a1 antagonist
Yohimbine
Selective a2 anatagonist
Prazosin
a1 antagonist, dilates arterioles and venous circulation, decreases preload and afterload
Uses: treat hypertension, congestive heart failure, raynaud phenomenon, benign prostate hyperplasia
ASE: "first dose effect" (marked postural hypotension), fainting, dizziness, etc.
Yohimbine
a2 antagonist - increase NE release, no relevant clinical use. May improve male sexual function
Good antidote for clonidine toxicity
The non-selective B-blockers (beta 1/2 antagonist)
propranolol
nadalol
timolol
Uses for non-selelctive b blockers
antihyptensive (short term)
antiarrhythmic (supraventricular)
Antianginal
Hyperthyroidism
Open-angle Glaucoma (timolol)
Anxiety
Major ASE for B receptor antagonist
Cardiac related bradycardia, heart blocks, precipitate congestive heart failure
Bronchospasms
CNS - hallucinations, nightmares
Tiredness, dizziness
Potential hypoglycemia (delayed recovery from insulin induced hypoglycemia)
Abrupt withdrawl - receptor sensitivity and tacharrhytmias
B1 antagonist (major 'beta blockers")
Metoprolol
Atenolol
Esmolol
Nebivolol
Bisoprolol
What do B1 antagnoist do, ASE, etc.?
Treat hypertension, congestive heart failure (metoprolol), angina, arrhythmias
ASE: similar CNS effects of non-selective B blockers (vivid dreams, insomnia. BUT, no bronchoconstriciton and less vasoconstriction (no B2 block)
B2 antagonist:
Butoxamine -
Which beta blockers are lipophillic?
Propranolol, this drug also has low oral bioavailabilty
What is the first cardioselective beta blocker?
Metoprolol
What can treat caffein overdose? Beta blockers, alpha blockers, or beta agonist, alpha agonist?
Beta blockers
This treats beta blocker toxicity
Glucagon
Combo adrenergic blockers to treat hypertenions and HF?
Carvedilol - ASE - fatigue
Labetalol - ASE - less tachycardia, doesn't treat CHF
What drugs treat CHF?
Metoprolol
Bisoprolol
Carvedilol