Term
(T/F) NE can inhibit is own release via negative feedback |
|
Definition
|
|
Term
Which transporter does it act on? |
|
Definition
|
|
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
|
|
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
|
|
Term
What are the two alpha adrenoceptors? |
|
Definition
|
|
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
|
|
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
|
|
Term
What is the sympathetic effect on vessels in smooth muscle? |
|
Definition
|
|
Term
How does epinephrine act at the alpha1/2 receptors, and the beta1/2 receptors? |
|
Definition
|
|
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
|
|
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
|
|
Term
What is the role of epinephrine in respiratory tract smooth muscle, and via which receptors? |
|
Definition
|
|
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
|
Definition
|
|
Term
What receptors does isoproterenol act on? |
|
Definition
|
|
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
|
|
Term
What is the result of this? |
|
Definition
|
|
Term
List the affinities of EPI, NE, INE, from highest to lowest, at the alpha receptors |
|
Definition
|
|
Term
List the affinities of EPI, NE, INE, from highest to lowest, at the beta1 receptor |
|
Definition
|
|
Term
List the affinities of EPI, NE, INE, from highest to lowest, at the beta2 receptors |
|
Definition
|
|
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
|
|
Term
Where does clonidine act? |
|
Definition
|
|
Term
|
Definition
It reduces neurotransmission to suppress SNS effects |
|
|
Term
|
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
|
|
Term
(T/F) Amphetamines achieve the same actions as NE in the periphery |
|
Definition
|
|
Term
|
Definition
To prevent sleep/suppress appetite/treat ADD |
|
|
Term
(T/F) Methylphenidate is a CNS stimulant similar to amphetamine |
|
Definition
|
|
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
|
|
Term
(T/F) It has both direct and indirect effects |
|
Definition
|
|
Term
|
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
|
|
Term
(T/F) Pseudoephedrine the active ingredient in Sudafed, which is a common medication taken to alleviate cold symptoms |
|
Definition
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
Definition
|
|
Term
What is the enzyme that metabolizes propranolol? |
|
Definition
|
|
Term
(T/F) The 4-OH metabolite is active |
|
Definition
|
|
Term
Name another important beta blocker |
|
Definition
|
|
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 |
|
|