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Autonomic Pharmacology - Sympathetic Pharmacology
Lomax yooo
87
Pharmacology
Undergraduate 3
05/30/2015

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Cards

Term
(T/F) NE can inhibit is own release via negative feedback
Definition
True
Term
Which transporter does it act on?
Definition
NET
Term
List all of the intermediates in the Epi/Norepi/Dompamine synthesis pathway
Definition
L Tyrosine -> L-DOPA -> Dopamine
-> Norepinephrine -> Epinephrine
Term
What causes parkinsons disease?
Definition
Dopamine deficiency
Term
How is L-DOPA used to treat Parkinsons?
Definition
Makes up for the dopamine deficiency - administered with decarboxylase inhibitor so that L-DOPA cannot get into the brain (cannot cross BBB)
Term
(T/F) Epinephrine is released by sympathetic ganglia
Definition
False, only by medulla
Term
What are the two alpha adrenoceptors?
Definition
Alpha 1 and Alpha 2
Term
Where is alpha1 found, what type of receptor is it, and how does it exert its effects?
Definition
- Blood vessels
- Gq/11 goupled
- Activates the PIP2 pathway
Term
What is the major action of Alpha1 receptors?
Definition
Vasoconstriction caused by the post-gang neuron
Term
Where is alpha2 found, what type of receptor is it, and how does it exert its effects?
Definition
- Some blood vessels, presynaptic (enteric and other)
- Gi- coupled
- Inhibits protein kinase and cAMP
Term
What are the 3 types of beta adreno-receptors?
Definition
Beta 1-3
Term
Where is beta1 found, what type of receptor is it?
Definition
- Heart, Kidney and Presynaptic neurons
- Signals via Gs receptor
Term
What is the function of beta1 in each location?
Definition
- Heart: controls heart rate (post synaptic)
- Kidney: controls renin release
Term
Where is beta2 found, what type of receptor is it?
Definition
- Bronchiolar, uterine, GI smooth muscle, skeletal muscle blood vessels
- Signals via Gs receptor
Term
What is the function of beta2 in each location?
Definition
- Bronchiolar, uterine, GI smooth muscle: relaxation
- Skeletal muscle blood vessels: vasodilation
- Immunosuppresion
Term
What are the 3 functions of beta3, and how does it signal?
Definition
- Lipolysis
- Smooth muscle relaxation
- Immunosuppresion
Term
What is the sympathetic effect on vessels in skeletal muscle?
Definition
Vasodilation
Term
What is the sympathetic effect on vessels in smooth muscle?
Definition
Vasoconstriction
Term
How does epinephrine act at the alpha1/2 receptors, and the beta1/2 receptors?
Definition
Agonistically
Term
What is its effect at beta 1?
Definition
Increase in heart rate and contractility
Term
Describe the effects of epinephrine on blood pressure at low and high concentrations
Definition
1. Low conc: Decrease in blood pressure
2. High conc: Increase in bp
Term
What receptor elicits the decrease in blood pressure at low [epi]?
Definition
Beta 2
Term
What receptors elicit the increase in blood pressure at high [epi]?
Definition
Alpha1 (primary), alpha 2, beta1
Term
What is the role of epinephrine in GIT smooth muscle, and via which receptors?
Definition
Inhibition, via alpha 2 and beta 2
Term
What is the role of epinephrine in uteral smooth muscle, and via which receptors?
Definition
Relaxation, beta 2
Term
What is the role of epinephrine in respiratory tract smooth muscle, and via which receptors?
Definition
Relaxation, Beta 2
Term
What are the metabolic effects upon epinephrine release?
Definition
1. Increase of blood glucose levels
2. Increase in free fatty acid
Term
What 3 things mediates this?
Definition
1. Glycogenolysis
2. Insulin
3. Glucagon
Term
How is the free fatty acid concentration increased?
Definition
By activating triglyceride lipase
Term
Which 3 receptors does Nor-Epi act on?
Definition
Alpha 1/2, Beta 1 (NOT beta2)
Term
What are its effects at beta1?
Definition
Increase in heart rate and contractility - increases BP
Term
What are its effects at alpha1/2?
Definition
Vasoconstriction - increases BP
Term
What is Isoproterenol?
Definition
Modified norepinephrine
Term
What receptors does isoproterenol act on?
Definition
Beta 1/2
Term
What does it do to beta 1?
Definition
Increases heart rate and contractility
Term
(T/F) Increases in heart rate and contractility by isoproterenol cause chronic BP elevation
Definition
False, these responses cause an acute increase in blood pressure
Term
What does it do to beta 2?
Definition
Vasodilation
Term
What is the result of this?
Definition
Decreased BP
Term
List the affinities of EPI, NE, INE, from highest to lowest, at the alpha receptors
Definition
Epi > NE >> INE
Term
List the affinities of EPI, NE, INE, from highest to lowest, at the beta1 receptor
Definition
INE > EPI = NE
Term
List the affinities of EPI, NE, INE, from highest to lowest, at the beta2 receptors
Definition
INE > EPI >> NE
Term
List 4 things that alpha agonists are used for/to treat
Definition
1. BP, or BP in shock (treats a sudden decrease)
2. Nasal decongestion
3. Hemmorrhage
4. Anaphylactic shock
Term
List 3 things that beta agonists are used for/to treat
Definition
1. Congestive heart failure (Beta1) 2. Asthma (Beta2) 3. Anaphylactic shock
Term
(T/F) Clonidine is an adrenoceptor agonist that acts at alpha2
Definition
True
Term
Where does clonidine act?
Definition
Brain and periphery
Term
What does it do?
Definition
It reduces neurotransmission to suppress SNS effects
Term
What is it used as?
Definition
An antihypertensive, and an antiadrenergenic
Term
What is its function/mechanism of action at low concentration?
Definition
Decreases SNS presynaptically, which reduces NE transmission
Term
What is its function/mechanism of action at high concentration?
Definition
Causes post synaptic vasoconstriction, which increases blood pressure
Term
Name 4 other beta adrenoceptor agonists, and which receptor they act on
Definition
1. Dobutamine (Beta1) 2. Dopamine (Beta1) 3. Salbutamol (Beta2) 4. Ritodrine (Beta2)
Term
What is ritodrine used for?
Definition
To arrest premature labour
Term
How do cocaine and tricyclic anti-depressants inhibit NE uptake?
Definition
Inhibits reuptake after synapsis - inhibits NET
Term
Name 4 indirect acting sympathomimetics
Definition
1. Amphetamine 2. Methylphenidate 3. Ephedrine 4. Pseudoephedrine
Term
What does amphetamine do?
Definition
Releases NE and other amines
Term
Where do amphetamines have their most potent effects?
Definition
In the CNS
Term
(T/F) Amphetamines achieve the same actions as NE in the periphery
Definition
True
Term
What are they used for?
Definition
To prevent sleep/suppress appetite/treat ADD
Term
(T/F) Methylphenidate is a CNS stimulant similar to amphetamine
Definition
True
Term
Why is it used preferentially to treat children with ADHD?
Definition
Because it has less impact on growth, since it does not suppress appetite
Term
What is the source of ephedrine?
Definition
Various plants
Term
(T/F) It has both direct and indirect effects
Definition
True
Term
How does it act?
Definition
As a alpha and beta agonist, and evokes the release of NE
Term
(T/F) It has a short duration of action
Definition
False, it has a long duration
Term
(T/F) It has a low potency
Definition
True
Term
(T/F) Pseudoephedrine the active ingredient in Sudafed, which is a common medication taken to alleviate cold symptoms
Definition
True
Term
Name 3 common mechanisms of action for sympatholytics
Definition
1. Receptor antagonists 2. NE synthesis inhibition 3. Inhibition of vesicular transporter
Term
Name the two types of sympatholytics
Definition
1. Adrenoceptor antagonists (post synaptic)
2. Other (presynaptic)
Term
What usually acts as as adrenoceptor antagonists?
Definition
Receptor blocking agents
Term
List 3 ways "other" presynaptic sympatholytics act
Definition
1. Synthesis inhibitor
2. Release inhibitor
3. NE depletor
Term
(T/F) Antagonists are the most important sympatholytic drugs
Definition
True
Term
Name 3 prototypical drugs, and which receptors they act on
Definition
1. Phentolamine (alpha1/2 antag)
2. Prazosin (alpha1 antag)
3. Propranolol (beta1/2 antag)
Term
(T/F) When an antagonist is administered, its immediate effect depends on the existing stimulation of receptors
Definition
True
Term
What two cardiovascular problems is it used to treat?
Definition
1. Hypertension
2. Congestive heart failure
Term
What are the adverse effects of alpha antagonists?
Definition
1. Orthostatic hypotension
2. Increased GI activity
3. Impaired ejaculation
4. Nasal stuffiness
Term
How does propranolol act at beta1/2 receptors?
Definition
Competitive antagonist
Term
What are its effects on the CVO?
Definition
Descreased heart-rate, vasodilation, decreased BP
Term
Name the 3 therapeutic uses of propranolol
Definition
1. Hypertension mechanisms
2. Ischemic heart disease
3. Arrhythmias
Term
Name the 3 adverse effects of beta antagonsits
Definition
1. Bronchoconstriction
2. Congestive heart failure (Underlying cardiac function that is compensated for by SNS activity, this compensation stops and patient may have heart failure)
3. Bradycardia
Term
List the pharmacokinetc properties of propranolol (5)
Definition
1. Lipid soluble - well absorbed
2. 90% plasma protein bound
3. Variable bioavailibility
4. Large Vd
5. Eliminated by hepatic metabolism
Term
What is its half life?
Definition
~4 hours
Term
What is the enzyme that metabolizes propranolol?
Definition
Cyp 2D6
Term
(T/F) The 4-OH metabolite is active
Definition
True
Term
Name another important beta blocker
Definition
Pindolol
Term
Why is pindolol often used?
Definition
It has a much larger bioavailibility
Term
Name 3 reasons why you would choose an alternative beta blocker?
Definition
1. If drug effect is complicated by lvier disease or metabolic drug interactions
2. May require a short duration of action
3. May desire selectivity for cardiac effect
Term
How does Metyrosine (alpha-methylparatyrosine) act as a sympatholytic?
Definition
Inhibiting NE synthesis by inhibiting tyrosine uptake, and by ihibiting VMAT
Term
What is the role of reserpine in NE inhibition?
Definition
Reserpine inhibits the transport of DA and NE into the synaptic vesicle, therefore inhibiting release
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