Term
| Where are alpha1 recepts? |
|
Definition
| most vascular smooth muscle, pupillary dilator, pilomotor sm musc, prostate, heart |
|
|
Term
| most vascular smooth muscle, pupillary dilator, pilomotor sm musc, prostate, heart - these have which type of alpha receptor? |
|
Definition
|
|
Term
| What would be the effects of alpha 1 stimulation? |
|
Definition
| contraction of most vascular smooth muscle, pupil dilation, pilomotor erection, prostate contraction, increased force of heart contraction |
|
|
Term
| contraction of most vascular smooth muscle, pupil dilation, pilomotor erection, prostate contraction, increased force of heart contraction - if I want to achieve these effects, which receptor should I stimulate? |
|
Definition
|
|
Term
| Where are alpha 2 recepts? |
|
Definition
| postsyn CNS adrenoreceptors, platelets, adrenergic and cholinergic nerve terminals, some vascular smooth musc, fat cells |
|
|
Term
| postsyn CNS adrenoreceptors, platelets, adrenergic and cholinergic nerve terminals, some vascular smooth musc, fat cells -- which alpha receptor would I find in these locations? |
|
Definition
|
|
Term
| What would be the effects of alpha2 stimulation? |
|
Definition
| platelet aggregation, inhibit NT release at adrenergic and cholinergic nerve terminals, contraction of some vascular smooth muscle, inhibition of lipolysis |
|
|
Term
| platelet aggregation, inhibit NT release at adrenergic and cholinergic nerve terminals, contraction of some vascular smooth muscle, inhibition of lipolysis -- if I want to achieve these effects, which receptor should I stimulate? |
|
Definition
|
|
Term
| Where would I find b1 recepts? |
|
Definition
| heart, juxtaglomerular cells |
|
|
Term
| Which type of b receptor would I find on heart and juxtaglomerular cells? |
|
Definition
|
|
Term
| What would be the effects of b1 stimulation? |
|
Definition
| increased force and rate of heart contraction, increased renin release |
|
|
Term
| stimulation of which receptor would cause increased force and rate of cardiac contraction and increased renin release? |
|
Definition
|
|
Term
| Where would I find b2 recepts? |
|
Definition
| respiratory, uterine, and vascular sm musc, skeletal muscle and liver |
|
|
Term
| which b receptor would I find on respiratory, uterine, and vascular sm musc, skeletal muscle, and liver? |
|
Definition
|
|
Term
| what would be the effects of b2 stimulation? |
|
Definition
| smooth muscle relaxation (respiratory, uterine, vascular), promotes K+ uptake from skeletal muscle, activates glycogenolysis in liver |
|
|
Term
| I want to achieve these effects: smooth muscle relaxation (respiratory, uterine, vascular), promote K+ uptake from skeletal muscle, activate glycogenolysis in liver. Which receptor should I stimulate? |
|
Definition
|
|
Term
| Where would I find b3 recepts? |
|
Definition
|
|
Term
| which alpha and which beta receptor is present on fat cells? What are their actions? |
|
Definition
| alpha2 - inhibits lipolysis, beta 3 - activates lipolysis |
|
|
Term
| which beta receptor is present on fat cells? |
|
Definition
|
|
Term
| which receptor mediates the activation of lipolysis? |
|
Definition
|
|
Term
| Where would I find D1 recepts? |
|
Definition
|
|
Term
| smooth muscle has which dopamine receptor? |
|
Definition
|
|
Term
| What is the effect of D1 stimulation? |
|
Definition
| dilates renal blood vessels |
|
|
Term
| Which receptor acts to dilate renal blood vessels? |
|
Definition
|
|
Term
| Where would I find D2 receptors? |
|
Definition
|
|
Term
| nerve endings have which type of D recept? |
|
Definition
|
|
Term
| What is the effect of D2 recepts? |
|
Definition
| modulates NT release from nerve endings |
|
|
Term
| which recept modulates NT release from nerve endings? |
|
Definition
|
|
Term
|
Definition
|
|
Term
| What types of drugs are midodrine and phenylephrine? |
|
Definition
|
|
Term
|
Definition
| activates PLC -> ^ intracellular Ca+ and vasocontriction |
|
|
Term
| Which drug activates PLC -> ^ intracellular Ca+ and causes vasocontriction? |
|
Definition
|
|
Term
|
Definition
| vascular smooth muscle contraction increasing BP |
|
|
Term
| which drug causes vascular smooth muscle contraction, increasing BP? |
|
Definition
|
|
Term
|
Definition
| activates PLC -> ^ intracellular Ca+ and vasocontriction |
|
|
Term
| effects of phenylephrine? |
|
Definition
| vascular sm musc contraction, increasing BP |
|
|
Term
| clinical application of midodrine? |
|
Definition
|
|
Term
| which drug is used for orthostatic hypotension? |
|
Definition
|
|
Term
|
Definition
| supine hypertension, piloerection, urinary retention |
|
|
Term
| Which drug's toxicity includes supine hypertension, piloerection, urinary retention? |
|
Definition
|
|
Term
| What is phenylephrine used for? |
|
Definition
| short term maintenance of BP in acute hypotension and intranasally to produce local vasocontriction as a decongestant |
|
|
Term
| which drug is used for short term maintenance of BP in acute hypotension and intranasally to produce local vasocontriction as a decongestant? |
|
Definition
|
|
Term
|
Definition
| clonidine, a-methyldopa, dexmedetomidine, tizanidine, apraclonidine, brimonidine |
|
|
Term
| Name the drug class: clonidine, a-methyldopa, dexmedetomidine, tizanidine, apraclonidine, brimonidine |
|
Definition
|
|
Term
|
Definition
| inhibits adenylyl cyclase, interacts with other intracellular pathways |
|
|
Term
| Which drugs inhibit adenylyl cyclase, and interact with other intracellular pathways? |
|
Definition
| clonidine (a2 agonists) and bromocriptine (D2 agonist) |
|
|
Term
|
Definition
| vasocontriction is masked by a central sympatholytic effect, which lowers BP |
|
|
Term
| Which drug causes masking of vasocontriction by a central sympatholytic effect, lowering BP? |
|
Definition
|
|
Term
| clinical applications of clonidine? |
|
Definition
|
|
Term
| which drugs are used in HTN? |
|
Definition
| clonidine (a2 agonist) and fenoldopam (D1 agonist) |
|
|
Term
| how is clonidine given? tox? |
|
Definition
| oral, transdermal, dry mouth and sedation |
|
|
Term
| which drug is given orally and transdermally, and produces dry mouth and sedation? |
|
Definition
|
|
Term
| What is a-methyldopa? How is it used, generally? |
|
Definition
| a2 agonist, central sympatholytic |
|
|
Term
| What is guanfacine? How is it used, generally? |
|
Definition
| a2 agonist, central sympatholytic |
|
|
Term
| What is guanabenz? How is it used, generally? |
|
Definition
| a2 agonist, central sympatholytic |
|
|
Term
| What are a-methyldopa, guanfacine and guanabenz? How are they used, generally? |
|
Definition
| a2 agonist, central sympatholytic |
|
|
Term
| name the drugs used as central sympatholytics. What is their MOA? |
|
Definition
| clonidine, a-methyldopa, guanfacine, guanabenz. a2 agonists. |
|
|
Term
| What is dexmedetomidine? MOA? What's it used for? |
|
Definition
| a2 agonist, prominent sedative effects and used in anesthesia |
|
|
Term
| Which drug is an a2 agonist with prominent sedative effects and is used in anesthesia? |
|
Definition
|
|
Term
| What is tizanidine? How is it used? |
|
Definition
| a2 agonist, used as muscle relaxant |
|
|
Term
| Name an a2 agonist used as a muscle relaxant |
|
Definition
|
|
Term
| What are apraclonidine and brimonidine? What are they used for? |
|
Definition
| Used in glaucoma to reduce IOP |
|
|
Term
| Name two a2 agonist drugs used in glaucoma to reduce IOP |
|
Definition
| apraclonidine, brimonidine |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| activates adenylyl cyclase, increases myocardial contractility |
|
|
Term
| name a drug that activates adenylyl cyclase to increase myocardial contractility |
|
Definition
|
|
Term
| what is the effect of dobutamine? |
|
Definition
| positive inotropic effect |
|
|
Term
| name a drug with a positive inotropic effect on the heart |
|
Definition
|
|
Term
| clinical applications for dobutamine? |
|
Definition
| cardiogenic shock, acute heart failure |
|
|
Term
| which drug is used in cardiogenic shock and acute heart failure? |
|
Definition
|
|
Term
| How do you give dobutamine? |
|
Definition
| IV, need to titrate dose for desire effect |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| activates adenylyl cyclase |
|
|
Term
|
Definition
| bronchial sm musc dilation |
|
|
Term
| which drug causes bronchial sm musc dilation? |
|
Definition
|
|
Term
| clinical applications for albuterol? |
|
Definition
|
|
Term
| which drug is used for asthma? |
|
Definition
|
|
Term
| how is albuterol given? tox? |
|
Definition
| inhalation, tremors, tachy |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| activates adenylyl cyclase |
|
|
Term
| which drugs in this chapter activate adenylyl cyclase? |
|
Definition
| dobutamine (b1 agonist), albuterol (b2 agonist), fenoldopam (D1 agonist) |
|
|
Term
| which drugs in this chapter inhibit adenylyl cyclase? |
|
Definition
| clonidine (a2 agonist), bromocriptine (D2 agonist) |
|
|
Term
|
Definition
| vascular smooth muscle relaxation |
|
|
Term
| which drug causes vascular smooth muscle relaxation? |
|
Definition
|
|
Term
| what is fenoldopam used for? |
|
Definition
|
|
Term
| What's special about dosing fenoldopam? |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| inhibits adenylyl cyclase and interacts with other intracellular pathways |
|
|
Term
| effects of bromocriptine? |
|
Definition
| restores dopamine actions in the CNS |
|
|
Term
| clinical applications for bromocriptine? |
|
Definition
|
|
Term
| How is bromocriptine given? Tox? |
|
Definition
| orally, nausea, HA, ortho hypo |
|
|
Term
| Which receptors use cAMP? |
|
Definition
|
|
Term
| Which receptors use ^ IP3, DAG? |
|
Definition
|
|
Term
| Which intracellular messenger do a2 receptors use? Increase or decrease? |
|
Definition
|
|
Term
| Which intracellular messenger do beta receptors use? Increase or decrease? |
|
Definition
|
|
Term
| Which intracellular messenger do D receptors use? Increase or decrease? |
|
Definition
| cAMP. D1 and D5 increase cAMP, D2/3/4 decrease cAMP. |
|
|
Term
| Does isoproterenol prefer b1 or b2 recepts? |
|
Definition
|
|
Term
| Which recepts does epi stimulate? |
|
Definition
|
|
Term
| Which recepts does norepi stimulate? |
|
Definition
|
|
Term
| What's the difference between homologous and heterologous desensitization? |
|
Definition
| homologous results in decreased response to only that specific receptor, hetero results in desensitization of another receptor as well |
|
|
Term
| A major mechanism of desensitization that occurs rapidly involves... |
|
Definition
| phosphorylation of receptors by members of the GRK family (homologous) |
|
|
Term
| Phosphorylation of an adrenoceptor by GRK enhances their affinity for... |
|
Definition
|
|
Term
| Arrestin interacts with... |
|
Definition
| clathrin and clathrin adaptor AP2 --> endocytosis of receptor |
|
|
Term
| maximal a and b activity is found with _______s, which have ____ groups on the __ and __ positions of the benzene ring |
|
Definition
| catecholamines, -OH, 3, 4 |
|
|
Term
| Why aren't catecholamines active orally? |
|
Definition
| they are inactivated by COMT, found in the gut and liver |
|
|
Term
| Absence of one of the -OH groups on a catecholamine has what effect? |
|
Definition
| improves bioavailability, prolongs DOA, increases distribution to CNS |
|
|
Term
| Absence of one of the -OH groups on a catecholamine has what effect? |
|
Definition
| improves bioavailability, prolongs DOA, increases distribution to CNS |
|
|
Term
| Substitution on the amino group of a catecholamine has what effects? |
|
Definition
| better at b-receptors, worse at a-receptors |
|
|
Term
| Substitutions on the alpha-carbon of catecholamines has what effect? |
|
Definition
| block oxidation by MAO, prolong action - e.g. ephedrine and amphetamine |
|
|
Term
| Substitution at the beta carbon of a catecholamine has what effect? |
|
Definition
| facilitates activation of adrenoreceptors, may be important for storage in vesicles |
|
|
Term
| phenylephrine ____s BP and ___s heart rate |
|
Definition
| increases, decreases (baroreceptor-vagal reflex) |
|
|
Term
| The important effect for a2 receptors is... |
|
Definition
| to produce CENTRAL inhibition of sympathetic tone and BP, which overrides the local effects to constrict blood vessels |
|
|
Term
| In patients with autonomic failure, clonidine may ____ BP |
|
Definition
|
|
Term
| beta receptor activation results in increased ____ influx in cardiac cells |
|
Definition
|
|
Term
| IV administration of dopamine promotes... |
|
Definition
| vasodilation of renal, splanchnic, coronary, cerebral, and perhaps other resistance vessels |
|
|
Term
| Dopamine actives ___ recepts in the heart |
|
Definition
|
|
Term
| At higher rates of infusion, dopamine activates vascular ___ recepts, leading to ___ |
|
Definition
|
|
Term
| In the eye, the radial pupillary dilator muscle contains ___ recepts |
|
Definition
|
|
Term
| a-agonists increase the outflow of aqueous humor and can be used to... |
|
Definition
|
|
Term
| b-ANTAGONISTS have what effect in glaucoma? |
|
Definition
| decrease production of aqueous humor |
|
|
Term
| the bladder base, urethral sphincter and prostate contain ___ recepts that mediate ____ |
|
Definition
| a, contraction and continence |
|
|
Term
| which is a centrally acting a2 agonist useful for sedation of intubated pts during treatment in the ICU, and also reduces requirements for opioids in pain control? |
|
Definition
|
|
Term
| xylometazoline and oxymetazoline are direct ___ agonists |
|
Definition
|
|
Term
| when used in large doses, oxymetazoline can cause ____ due to central effect |
|
Definition
|
|
Term
| Which drug is a potent vasodilator, causes increased cardiac output, fall in diastolic, lesser decrease or slight increase in systolic? |
|
Definition
|
|
Term
| what is a partial b1 agonist? |
|
Definition
|
|
Term
| What is found in ma huang? |
|
Definition
|
|
Term
| ___ is a racemic mixture of phenylisopropylamine |
|
Definition
|
|
Term
| Which drug is like amphetamine, has been promoted as an anorexiant and is a popular drug of abuse? |
|
Definition
|
|
Term
| Which drug is a psychostimulant with effects on NE, D, serotonin, glutamate, and decreases GABA, and is used in narcolepsy? |
|
Definition
|
|
Term
| Atomoxetine and reboxetine are... |
|
Definition
|
|
Term
| Which drug is an inhibitor of serotonin and NE reuptake, and is the only appetite suppressant approved by the FDA for long term tx of obesity? |
|
Definition
|
|
Term
| ____ is a local anesthetic with peripheral sympathomimetic action that results from inhibition of transmitter reuptake at noradrenergic synapses |
|
Definition
|
|
Term
| the major action of cocaine in the CNS is... |
|
Definition
| inhibit dopamine reuptake in the pleasure centers |
|
|
Term
| For acute hypotension, which drugs have been used? |
|
Definition
| norepi, phenylephrine, methoxamine |
|
|
Term
| b2-selective agents relax the pregnant uterus, so drugs like ___ and ____ suppress premature labor |
|
Definition
|
|
Term
| Epinephrine and dipivefrin are used for |
|
Definition
|
|
Term
| longer acting b2 agonist for prevention of asthma attacks? |
|
Definition
|
|
Term
| ___ agonists may be useful in acute heart failure |
|
Definition
|
|
Term
| These agents decrease blood flow or increase blood pressure, are local decongestant, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion |
|
Definition
|
|
Term
| Shock due to septicemia or myocardial infarction is made worse by |
|
Definition
| Increasing afterload and tissue perfusion declines |
|
|
Term
| Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus |
|
Definition
|
|
Term
| Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| sinus tachy and arrhythmias |
|
|
Term
|
Definition
|
|
Term
| The selective agents lose their selectivity at |
|
Definition
|
|
