Lecture 79 Flashcards

1
Q

The ______ nervous system innervates vascular smooth muscle, whereas the _____ nervous system does not.

A

SYMPATHETIC innervates, whereas PARASYMPATHETIC does not.

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2
Q

Activation of alpha1 receptors on vascular smooth muscle causes _______, while activation of beta2 receptors causes ______. When both alpha1 and beta2 receptors are activated, the effect of _____ is dominant.

A

Alpha1 activation causes VASOCONSTRICTION, while activation of beta2 causes VASODILATION. The effect of ALPHA1 is dominant.

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3
Q

There are muscarinic receptors in the vascular smooth muscle, but no Parasymp innervation. Instead, locally produced ____ can bind muscarinic receptors on vascular smooth muscle causing _____.

A

ACh

VASODILATION

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4
Q

The bronchial smooth muscle contains beta2 receptors for ____ innervation and muscarinic receptors for ____ innervation. Actiavtion of beta2 receptors cause ______, whereas activation of muscarinic causes _____ and mucous formation.

A

beta2 for SYMPATHETIC and Muscarinic for PARASYMPATHETIC. Activation of beta2 causes BRONCHODILATION, whereas activation of muscarinic causes BRONCHOCONSTRICTION and mucous formation.

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5
Q

Sympathetic activation of beta2 receptors on GI tract smooth muscle ______ contraction/peristalsis and defecation, while Parasympathetic activation of muscarinic receptors does the opposite.

A

DECREASES peristalsis and defecation

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6
Q

Sympathetic activation of alpha1 receptors on sphincters causes _____ while Parasympathetic activation of muscarinic receptors on sphincters causes _____.

A

Sympathetic activation causes CONTRACTION while Parasympathetic activation causes RELAXATION.

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7
Q

The uterus has alpha1 and beta2 receptors, activation of which cause ____ contractions and ____ contractions respectively.

A

alpha1 INCREASES contractions, beta2 DECREASES contractions.

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8
Q

Activation of alpha1 and beta2 receptors in Salivary glands increase _____ secretions, whereas activation of Muscarinic receptors increases ______ secretions.

A

Activation of alpha1 and beta2 increase VISCOUS secretions, whereas activation of Muscarinic increases WATERY secretions.

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9
Q

The prejunctional Neural uptake transporter on postganglionic adrenergic neurons is responsible for about 95% of the uptake of ____ while the postjunctional extraneuronal transporter is only responsible for about 5%. If taken back into the neuron, ____ can be broken down by _____, or repurposed. If taken into the effector cell (post-junctional), it can be broken down by ____ or ____.

A

Prejunctional neuronal uptake transporters are responsible for about 90% of NE uptake.

If taken back into the neuron, NE can be broken down by MAO or repurposed. In effector cell, it can be broken down by MAO or COMT.

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10
Q

Direct acting Adrenergic Agonists bind to receptors on _____, while indirect acting adrenergic agonists _____ levels of NE.

A

Bind to receptors on EFFECTOR, while indirect INCREASE levels of NE.

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11
Q

Epi is a _____-selective adrenergic agonist, meaning it can bind to all adrenergic receptors. However, it preferentially binds ____ receptors (they have greater affinity), so at low doses it would cause vaso______, and thus a ______ (increase or decrease?) in diastolic BP. Which receptors does it bind in the heart, and what does that mean for CO and systolic BP? Keep in mind any catecholamine must be injected; if taken orally, they would be broken down by ____ in the GI tract.

A

Epi is NON-selective.

Beta2

Dilation

Decrease in diastolic

It binds Beta1 in the heart, so increase in CO and systolic BP

Any catecholamine must be injected because they can be broken down by MAO in the GI tract.

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12
Q

Epi can activate beta2 receptors on hepatocytes, signalling breakdown of _____.

A

Breakdown of GLYCOGEN.

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13
Q

Epi is indicated for treatment of ____ emergencies and hypersensitivity reactions (anaphylaxis.) It is also co-administered with local _____ because of its vaso_____ effects at higher than endogenous doses. Epi can be used to treat glaucoma bc it reduces the amount of aqueous humor produced, but it is contraindicated in patients with ___-___ glaucoma. Why?

A

Treatment of CARDIAC emergencies –> increases both systolic and diastolic BP. It is also co-administered with local ANESTHETICS because of its VASOCONSTRICTION effect at higher than endogenous doses.

Closed-angle glaucoma –> alpha1 receptors would be activated –> dilation of the pupil –> worsening the drainage of aqueous humor into the canal of Schlemm.

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14
Q

NE is a selective adrenergic agonist and binds all adrenergic receptors EXCEPT _____2.

A

Except BETA2

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15
Q

DA is also selective, and binds only ___ and ___ adrenergic receptors. It also binds DA receptors on vascular endothelium, causing vaso______ at low doses. This is overridden by its binding to _____1 receptors at high doses, leading to vaso____ EXCEPT in renal arteries –> a nice healthy blood flow is maintained to the kidneys.

A

DA binds only ALPHA1 and BETA1 adrenergic receptors. It also binds DA receptors on vascular endothelium, causing VASODILATION at low doses. This is overridden by its binding to ALPHA1 receptors at high doses, leading to VASOCONSTRICTION.

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16
Q

Dobutamine is selective for all adrenergic receptors EXCEPT ____2. Typically, it’s given for its agonist effect on beta1 receptors. This is the drug that’s used for people who can not exercise during cardiac stress tests.

A

Except ALPHA2.

17
Q

Phenylephrine is an ___1 agonist, and its most common use is as a nasal _____, though it can be used to treat _____tension and “blood-shot” eyes. It is contraindicated in people with hypertension.

A

Phenylephrine is an ALPHA1 agonist, and its most common use is as a nasal DECONGESTANT, though it can be used to treat HYPOtension and blood-shot eyes.

18
Q

Clonidine is an ____2 agonist, and its actions are almost exclusively observed in the _____, rather than the periphery. It is considered a ____ -line drug to treat hypertension, as are ALL ____2 AGONISTS. It acts to _____ overall sympathetic tone by activating these receptors in the brain. As a result, systolic and diastolic BP ______ (so it can be used to treat hypertension). Keep in mind it can be used to treat withdrawal symptoms, as these are associated with increased sympathetic tone. Clonidine is administered ______, and abrupt withdrawal can lead to rebound-______. It was discovered that ____2 agonists can be used to treat _____, as they reduce the production of Aqueous Humor. _____ is one such drug, and is preferred over others because it doesn’t irritate the eye.

A

Clonidine is an ALPHA2 agonist, and its actions are almost exclusively observed in the CNS rather than in the periphery. It is considered a SECOND-line drug, as are ALL ALPHA2 AGONISTS. It acts to DECREASE overall sympathetic tone by activating these receptors in the brain. As a result, systolic and diastolic BP DECREASE. Administered ORALLY, and abrupt withdrawal can lead to rebound-HYPERTENSION. ALPHA 2 agonists can be used to treat GLAUCOMA. BRIMONIDINE is one such drug.

19
Q

Albuterol is a selective ____2 agonist used to treat _____. It is preferred over other ____ agonists because it is selective for ____2 –> no effect on heart.

Some of the side effects of Beta2 agonists include _____glycemia because of their action on hepatocytes, and fine tremors.

There is concern correlated with overuse of Beta2 agonists because it may lead to ____-regulation of the receptor. Keep in mind the Beta2 receptor is a _____ (which type of receptor?) which can be internalized in a vesicle if overstimulated.

A

Albuterol is a selective BETA2 agonist used to treat ASTHMA. It is preferred over other BETA agonists because it’s selective for BETA2 –> no effect on heart.

HYPERglycemia

Overuse of Beta2 agonists may lead to DOWN-regulation of the receptor. Keep in mind it is a GPCR.

20
Q

_____ is a Beta2 agonist used to down-regulate contractions of the uterus.

A

TERBUTALINE

21
Q

Indirect acting adrenergic agonists –> work to increase levels of NE at effector cell junction. Amphetamine is one that binds to prejunctional uptake transporter and NE vesicle uptake transporter, causing both to _____ the direction of transports.

A

Causing both to REVERSE the direction of transport.

22
Q

_____ (Ritalin) is an alternative to amphetamine for treatment of ADHD with decreased effect on the periphery and risk of V-fib.

A

METHYLPHENIDATE

23
Q

Tyramine is a breakdown product of ______. It acts like amphetamine, so it increases NE release. People taking MAO inhibitors need to restrict their diets to avoid too much tyramine.

A

Tyrosine