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 |
|
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