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81 Cards in this Set
- Front
- Back
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L tyrosine |
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Levodopa not good solubility at ph = & used for Parkinsons - can pass BBB - central activity |
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Why does metyrosine inhibit? |
similar structure to L-tyrosine, competes and L-tyrosine can't bind |
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L-tyrosine to Levodopa |
Tyrosine hydroxylase - rate limiting step |
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Levodopa to Dopamine |
L-Aromatic amino acid decarboxylase |
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Dopamine - COOH removed can't cross BBB at ph 7 - highly ionized |
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Carbidopa Inhibitor similar to L-Dopa
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Why is Carbidopa used with levodopa? |
for parkinsons takes advantage of inhibition of enzyme to slow down L-dopa metabolism to dopamine = longer time to cross BBB |
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Norepinephrine Primary amine (addition of OH) |
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enzyme between Dopamine and Norepinephrine |
Dopamine B-hydroxylase |
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Functional group |
Catechol |
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Epinephrine secondary amine |
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enzyme between norepinephrine and epinephrine |
Phenylethanolamine N-methyltransferase (adrenal medulla) |
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R=H: Norepinephrine R=CH3: Epinephrine |
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MAO |
monoamine oxidase |
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COMT |
Catechol O-methyl transferase |
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Oxidation - forms aldehyde
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forms alcohol |
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methylation |
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Major metabolite of norepinephrine and epinephrine |
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Arterioles receptor type and response |
a1,a2 Constriction |
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Vascular smooth muscle receptor type and response |
B2, dilation |
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eye (radial muscle) receptor type and response |
a1, constriction (dilation) |
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Fat cells, receptor type and response |
a1, b3 lipolysis |
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heart receptor type and response |
B1 increased rate and force increased conduction velocity |
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intestine receptor type and response |
a1, B2 decreased motility |
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liver receptor type and response |
a1, b2 increased gluconeogenesis and glycogenolysis |
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lungs receptor type and response |
B2 relaxation |
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uterus receptor type and response |
a1, b2 contraction relaxation |
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a1 stimulation |
vasoconstriction |
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a2 stimulation |
decreased sympathetic activity (targets pre-synaptic) |
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B1 stimulation |
increase rate (chronotropic) and force (inotropic) of cardiac contratction stimulate renin secretion |
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B2 stimulation |
smooth muscle relaxation bronchodilation vasodilation glycogenolysis |
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b3 stimulation |
adipose tissue, increase lipolysis |
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D1 stimulation |
dilation of renal blood vessels |
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precursor for neurotransmittors |
tyrosine |
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A1 agonist indications |
nasal decongestants opthalmic vasoconstriction |
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B2 agonists |
bronchodilators (asthma) anaphylactic shock |
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a2 agonist indication |
glaucoma hypertension |
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B-phenylethylamine |
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catecholamine ionization at ph 7 |
98% |
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Catechol (isoproterenol) B selectivity |
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Resorcinol R1=CH(CH3)2: Metaproterenol
B2: no COMT` |
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meta-hydroxymethyl Albuterol: R1=C(CH3)3
B2: no COMT |
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only meta-OH Phenylephrine R1=CH3
a1 |
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Norepinephrine Direct acting
a, B1 agonist IV - not orally active hypotensive emergency air-oxidized to o-quinone |
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Epinephrine direct acting easily oxidized a,B1, B2 agonist not orally active
nasal decongestant, local anesthetics asthma, anaphylactic
open-angle glaycoma - epinephryl borate |
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Dipiverferin direct acting
glaucoma: alpha 2 lipophilic activated by esterase's (prodrug) |
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Dopamine no b-hydroxy
Renal D1-receptor agonist - renal vessel dilation direct and indirect B1-agonist treatment of shock: increase BP and HR IV |
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Phenylephrine direct acting a1 agonist - vasoconstrictor
used for hypotensive shock mydriatic and glaucoma active orally no CNS stimulation |
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Methoxamine direct acting a1 agonist - vasoconstrictor
maintain adequate arterial BP in surgery |
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General structure of imidazoline a-agonist (direct acting) |
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Naphazoline direct acting alpha1 agonist
nasal and opthalmic decongestant pka-10 (at ph 7, over 99% ionized, no CNS activity)
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Tetrahydrozoline
direct acting alpha1 agonist
nasal and opthalmic decongestant pka-10 (at ph 7, over 99% ionized, no CNS activity) |
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Xylometazoline
direct acting alpha1 agonist
nasal and opthalmic decongestant pka-10 (at ph 7, over 99% ionized, no CNS activity) |
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Oxymetazoline
direct acting alpha1 agonist
nasal and opthalmic decongestant pka-10 (at ph 7, over 99% ionized, no CNS activity)
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Clonidine c
antihypertensive 1/2 life: 8-12hrs pka 8
good lipophilicity stimulate both a2-adrenoreceptors and imidazoline receptors in CNS
analgesic, ocular hypotensive effects |
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selective a2 agonists; direct centrally-acting imidazolidines |
activation of presynaptic a2-receptors, inhibit NE release, decrease sympathetic outflow and lower BP
(need access to CNS, must be centralyactive) |
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apraclonidine |
+ a para NH2 glaucoma pka: 9 t1/2 = 6 hrs
selective a2 agonist |
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Guanabenz selective a2 agonist
open ring imidazolidine antihypertensive 1/2 life = 6hr |
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Guanfacine selective a2 agonist
antihypertensive t1/2 = 17hrs |
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CNS a2 agonist Fenoldopam (phenylethylamine derivative)
Selective dopaminergic-D1 agonist, moderate affinity for a2-receptor
peripheral arteriolar dilator used for hypertensive crises
racemic mixture used, (R)-isomer active |
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Isopreterenol direct acting B-adrenergic agonist
B1=B2 potent bronchodilator, cardiac stimulant
inhale,inject, sublingual |
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Dobutamine direct acting dopamine analog
+isomer: b1 and b2 agonist
- isomer a1 agonis
racemic mixture stronger inotropic (strength of contraction) than chronotropic
CHF, surgery |
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Metaproteranol direct acting, selective B2 agonist
bronchodilator for asthma
active orally lower B2 affinity than isoproterenol, longer duration
bulkier R = more b2 selectivity |
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terbutaline |
R=C(CH3)3 B2 agonist |
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Albuterol selective B2-agonist
active orally long duration |
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Pirbuterol more lipophilic
selective B2-agonist |
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Salmeterol Ph=phenyl
much higher lipophilicity
selective b2-agonist |
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selective b2 agonist |
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Bitelterol - inhalation for bronchial asthma (prodrug) selective b2 agonist
colterol=active metabolite |
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Ephedrine direct and indirect acting a and b adrenergic agonist nasal decongestant, allergy, colds mild analeptic (CNS stimulant) antiasthmatic, oral, IV,IM, topical
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Hydroxyamphetamine
indirect acting adrenergic, release endogenous NE
lack benzylic hydroxyl or with inappropriate stereochemistry
OH on phenyl makes too polar to cross BBB |
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Pseudoephedrine nasal decongestant, many OTC preparations
indirect acting adrenergic, release endogenous NE
lack benzylic hydroxyl or with inappropriate stereochemistry
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