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Pharmacology Final
dr. rodgers
55
Pharmacology
Undergraduate 3
12/10/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
parasympathetic branch innervates:
Definition

cardiac and smooth muscle

gland cells

nerve terminals

Term

sympathetic innervates:

 

Definition

sweat glands

cardiac and smooth muscle

gland cells

nerve terminals

renal vascular smooth muscle

Term
somatic nerves innervate:
Definition

skeletal muscle

 

(nicotinic receptor --> ACh released)

Term
_______ nerves carry impulses away from the CNS to the target organs
Definition
efferent
Term
_______ nerves have LONG preganglionic fibers
Definition

Parasympathetic!

 

leaves cranial & sacral areas of the spinal cord

Term
______ is released in postganglionic neurons of the SYMPATHETIC nervous system.
Definition
Norepinephrine
Term
________ have SHORT preganglionic fibers
Definition
sympathetic nerves
Term
Parasympathetic receptors: postsynaptic? effector?
Definition

postsynaptic: Nicotinic receptor

 

effector: muscarinic

Term
ααααsympathetic receptors: postsynaptic? effector?
Definition

postsynaptic: nicotinic receptor

 

effector: (NE) α, β

Term
______ neurons exit the CNS from thoracolumbar region of the spinal cord
Definition
sympathetic
Term
_______ neurons exit the CNS from the craniosacral region
Definition
parasympathetic
Term
Preganglionic nerves of both branches of the ANS release ______.
Definition
ACh
Term
Al neurons that release ACh are called ____.
Definition
cholinergic
Term
Neurons that release NE are called ___.
Definition
adrenergic
Term
How are sweat glands an exception to the neurotransmitter rule?
Definition
They are sympathetically innervated; however, their postganglionic nerves are CHOLINERGIC (release ACh instead of NE) even though they are anatomically sympathetic (come out of the middle of the spinal cord)
Term
Certain blood vessels in the kidney are innervated by ___1___ nerves that release __2__ instead of NE. 
Definition

1) sympathetic

 

2) dopamine!

 

** Dopamine is a weak agonist on alpha and beta receptors, but also activates its own dopamine receptors in a more potent manner. **

Term
Example of autonomic nerves that are nonadrenergic and noncholinergic (NANC)
Definition

1)  Coprus cavernosum of the penis is innervated by nerves that release NO.  Release of NO acts on smooth muscle of the cavernosum, producing relaxation and engorgement with blood to produce an erection. 

2) Other NANC neurons release a variety of peptide and non-peptide transmitters (not just NO). Found in: GI tract, lungs, urinary tract, and CNS

Term
How is the adrenal gland an exception to the dual innervation rule?
Definition

Innervated exclusively by a preganglionic nerve but not a postganglionic nerve of the SYMPATHETIC nervous system.

 

Transmitter released: ACh

 

Enhanced release of ACh at adrenal medulla activates NICOTINIC receptors to increase secretion of EPI (adrenaline) by cromaffin cells into the bloodstream.

Term
The vast majority ofsmall arteries and arterioles are innervated only by the ____ branch of the ANS.
Definition

SYMPATHETIC!

 

arterioles = ALPHA receptors!!!

 

Blood flow and BP are controlled by the sympathetic nervous system.

 

Parasypathetic may influence flow in certain vascular beds, such as corpus cavernosum, but otherwise has little to no effect on blood flow or BP.

Term
Lungs (bronchi and bronchioles) are strongly innervated by the __1___ nervous system, but only weakly innervated by the ___2__ branch.
Definition

1) parasympathetic (ACh)

 

2) sympathetic

 

** SMC contraction cellular signal = Ca2+ moved inside by DAG, IP3**

Term
How do the few blood vessels innervated by the  parasympathetic n.s. respond to neurally-relased ACh?
Definition

Skeletal muscle, coronary arteries, corpus cavernosum...all respond LOCALLY by dilating due to release of NO from vascular endothelial cells.

 

But... injections of ACh and similar drugs cause systemic vasodilation because ALL endothelial cells have muscarinic receptors that are coupled to NO release.

 

However...if endothelium is removed from blood vessels, they will CONSTRICT (contract) in response to ACh bc of the action of ACh to stimulate M-1 receptors on the exposed smooth muscle

Term
Skeletal muscles are innervate by __1__ nerves which release __2__ and activate __3__ receptors.
Definition

1) somatomotor nerves

2) ACh

3) nicotinic

 

**Nm = nicotinic receptors of the somatomotor nervous system found on skeletal muscle.**

Term
A cholinergic junction illustrates:
Definition

1) synapses in all autonomic ganglia (sym & parasym)

2) the "synapse" btwn sym. preganglionic neurons & adrenomedullary cromaffin cells

3) parasym. neuroeffector junction

 

**↑ action potential frequency

↑ Ca2

↑ACh

Acetyl cholinesterase inhibitor = nerve gas

Term
What is the noradrenergic neuroeffector junction?
Definition

junction between sympathetic postganglionic neuron and an effetor cell

 

Tyrosine -> L-Dopa -> Dopamine

 

DβH converts Dopamine to NE

(pg. 16)

Term
Epinephrine can do two things:
Definition

1) stimulate alpha-1 to produce constriction (i.e. arterioles)

2) stimulate beta-2 to produce dilation

 

**Think of fight or flight response: You want to ↑ blood flow in the limbs but shunt blood flow in middle body (gut and gland)

Term
sympathomimetic
Definition

agonist drug that imitates effects of the sym. nervous system and thus acts like either NE or EPI

 

includes alpha and beta adrenoceptor agonists

Term
glycogenolysis
Definition

breakdown of glycogen to glucose

 

mainly in liver and skeletal muscle

Term
juxtaglomerular cells
Definition
specialized cells near the glomeruli in the kidney that secrete the enzyme renin into the bloodstream in response to neural and other influences
Term
relative potencies of NE (from postgang. neurons) and EPI (in blood from adr. medullary cromaffin cells) on different receptor subtypes 
Definition

alpha-1: NE>EPI

alpha-2: NE>>>>>EPI

beta-1: NE<EPI

beta-2: NE<<<<<EPI

Term

List the primary alpha-1 receptor mediated effects

(NE, EPI, and alpha agonist drugs)

Definition

CONSTRICTION OF:

arteriolar smooth mucle

genitourinary smooth muscle

radial muscle of eye

 

RELAXATION OF: intestinal smooth muscle

 

INCREASED GLYCOGENOLYSIS in liver

Term
Alpha-1 agonist drugs:
Definition

Alpha-1 SELECTIVE:

phenylephrine, methoxamine, mephentermine, metaraminol, tetrahydrozoline, naphazoline, mitodrine

 

NONSELECTIVE (w. some Beta activity):

dobutamine, ephedrine, pseudoephedrine, phenylpropanolamine

 

Term
Therapeutic uses of alpha agonist drugs:
Definition

- nasal decongestion (orally & topical in nasal sprays)

- local anesthetic preparations

- ocular anti-redness preparations

- hypersensitivity & anaphylaxis: (epinephrine = DOC)

Term
adverse effects of alpha agonist drugs
Definition

exteme elevation in BP

cerebrovascular accident

myocardial necrosis & infarction

Term

Predominantly BETA-2 mediated effects

 

(EPI or β agonist drugs)

Definition

RELAXATION OF:

arteriolar smooth muscle

bronchiolar smooth muscle

intestinal smooth muscle

uterine smooth muscle

ciliary muscle of eye

spleen capsule

 

INCREASED K+ UPTAKE in skeletal muscle

 

INCREASED INSULIN SECRETION in pancreatic islet beta cells

Term

Predominantly BETA-1 mediated effects

 

(EPI, NE, or β agonist drugs)

Definition

HEART SA Node: ↑HR (positive chronotropic effect)

 

HEART AV Node: ↑conduction velocity (pos. dromotropic effect)

HEART His-Purkinje cells: ↑conduction velocity & automaticity

 

HEART Atrial Muscle: ↑contractile force (pos. inotropic effect)

HEART Ventrical muscle: ↑contractile force

 

KIDNEY juxtaglomerular cells: ↑renin secretion

Term
BETA agonist drugs
Definition

Beta-2 Selective:

tertbutaline, metaproterenol, albuterol, isoetharine, perbuterol, fenoterol, salmeterol, ritodrine

 

Nonselective:

isoproterenol (no α activity), dobutamine, ephedrine, pseudophedrine, phenylpropanolamine (some α activity)

Term
therapeutic uses of beta agonist drugs
Definition

- anaphylactic shock (EPI = DOC)

- cardiogenic shock (low cardiac output, BP, or both); β agonists or fenoldopam

- Bronchospasm

- Cardiac Arrest (with alpha agonists)

 

Term
Adverse effects of beta agonist drugs
Definition

severe tachycardia & cardiac arrhythmias, angina pectoris, cardiac, necrosis and damage

 

skeletal muscle tremors

Term
dopamine
Definition

- neurotransmitter in brain and in autonomic neurons going to kidney

- activates its own receptors (D-1 and D-2) as well as alpha and beta adrenoceptors

- used to improve renal blood flow in conditions of shock (very low BP)

- Fenoldopam: Seceltive D-1 receptor agonist, also used in treating shock.

Term
Prazosin vs. Phentolamine
Definition

Prazosin:

- newer. Selective alpha-1 blocker.

- Causes vasodilation; bronchodilation for anaphylaxis

 

Phentolamine:

- older drug; nonselective a-1 and a-2 blocker.

- Inhibits NE to inhibit its own release, resulting in STIMULATION = more NE!

- more severe effects than prazosin

Term
common adverses effects of alpha blockers
Definition

fluid retention

 

tachycardia (BP↓, HR↑)

Term
Phenylephrine is a(n) ____ drug that causes ____.
Definition

Alpha agonist

 

vasoconstriction of arteriolar smooth muscle

decreased blood flow

Term
EPI stimulates ___ receptors and produces ____.
Definition

Alpha-1, beta-1, beta-2

 

vasoconstriction, decr. blood flow (a1)

positive inotropy (ventric. cardiomyocyte), ↑CO (B1)

bronchodilation (bron. sm. muscle), ↑air flow (B2)

Term
NE stimulates ____ receptors and causes ____.
Definition

alpha-1, alpha-2, beta-1

 

vasoconstriction, decr. blood flow (a1)

inhibits NE to inhibit own release (a2)

bronchodilation, ↑air flow (b2)

Term
Dobutamine
Definition

B-1 agonist

 

causes positive inotropy (ventricular cardiomyocyte)

increased cardiac output 

Term
Isoproterenol
Definition

nonselective beta agonist

 

positive inotrophy (vent. cardiomyocyte), ↑ CO (B!)

bronchodilation, ↑ air flow (B2)

Term
terbutaline
Definition

B-2 agonist used to treat asthma

effector: bronchiolar smooth muscle

signal: cAMP

causes: relaxation; therefore, opening airways

 

bronchodialtion, ↑ air flow

Term

Fenoldopam is useful for the treatment of ____.

 

Definition

cardiogenic and hypervolemic shock (severely reduced CO)

 

dopamine/fenoldopam have ability to selectively dilate renal blood vessels and ↑ renal blood flow

 

renal vasodilation helps maintain perfusion of kidneys when systemic BP or CO is very low

Term
What is the rationale for the therapeutic effects of alpha agonists on nasal decongestion?
Definition

congestion is caused by dilation of blood vessels, engorging & swelling mucosa of nasal passages

 

activation of alpha adrenoceptors on vascular s.m. in the vessels of the nasal mucosa causes blood vessels to constrict, counteracting the effect of vasodilation, and opening up nasal passages. 

Term
What is the therapeutic effect of alpha agonists used for local anesthetic preparations?
Definition

produce local vasoconstriction and restriction of systemic absorption, which has 2 major effects:

 

1) ↑duration & magnitude of anesthetic effect

2) decreases systemic toxicity of local anesthetic

Term
What is the rationale for therapeutic effect of alpha agonists used for ocular anti-redness?
Definition
Redness in the whites of the eyes is caused by vasodilation of the surface blood vessels, which is counteracted by vasoconstriction effects of alpha agonists
Term
What is the rationale for therapeutic effects of alpha agonists on anaphylactic shock?
Definition

Anaphylaxis is a mix of very low BP and constriction of upper airways produced by antigen-induced release of histamine

 

EPI counteracts low BP by producing systemic vasoconstriction (a1) and the bronchoconstriction by relaxing s.m. around airways (b2)

 

EPI also impedes release of histamine from mast cells (Beta effect)

Term

What are the rationales for adverse

effects of alpha agonists?

Definition

Extreme elevation in BP: usually caused by overdose; extreme effect of vasoconstriction

 

Cerebrovascular accident: vasoconst. of cerebral blood vessels

 

myocardial necrosis/infarction: extreme vasoconstr. of coronary microvessels

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