Term
What type of receptor has this order of potency:
Epi> NE>>>Iso |
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Definition
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Term
What type of receptor follows this order of potency:
Iso> Epi>>> NE |
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Definition
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Term
| Lands propposed B1 and B2 receptors. Where are they mainly located? |
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Definition
B1 = Heart
B2 = Smooth muscle |
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Term
| In 1974 Langer proposed __________ and __________ receptors. |
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Definition
Alpha 1 = postsynaptic
Alpha 2 = presynaptic |
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Term
| Arch propsed B3R. Where are they located? |
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Definition
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Term
| Alpha 1 Receptors stimulate which GPCR ? And what does this cause? |
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Definition
Gq = Increase IP3 and DAG
This releases Ca2+ to contract smooth muscles |
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Term
| Alpha2R stimulate which GPCR? And what does that cause? |
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Definition
Gi =
Decrease in cAMP and Increase in K+
This hyperpolarizes the membrane which causes the smooth muscles to relax |
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Term
| Beta R stimulate which GPCR? and what does it cause? |
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Definition
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Term
What type of receptor has this order of potency:
Epi> NE>>> ISO |
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Definition
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Term
What type of receptor has this order of potency:
ISO>Epi= NE |
|
Definition
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Term
What type of receptor has this order of potency:
ISO= NE>> Epi |
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Definition
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Term
| How do you distinguish between the different Alpha1 R? |
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Definition
| The length of the COOH tail |
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Term
| How do you distinguish between the different Alpha2 R? |
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Definition
| By the length of the NH2 tail on the outside |
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Term
| How do you distinguish between the different Beta R? |
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Definition
| They have different intracellular loops and different number of phosphorylation sites. |
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Term
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Definition
400-600 A.A lenth (NH2 end on outside, COOH end inside)
7 transmembrane spanning regions
3 extracellular loops
3 intracellular loops
Sites for protein dependent phosphorylation |
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|
Term
| Where are the critical residues for EPI binding? |
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Definition
TM 3 - Aspartate
TM 5 - Serine
TM6 - Phenylalanine |
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Term
| T/F: Receptors have absolute selectivity. |
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Definition
| False; they are dose dependent |
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Term
| What is the main therapeutic use of Alpha1 Agonist? |
|
Definition
Increase blood pressure
Nasal decongestant |
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Term
| What is the main therapeutic use of Beta1 Agonist? |
|
Definition
Facilitate cardiac function
(increase CO, HR and contractility) |
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|
Term
| What is the main therapeutic use of Alpha1 Antagonist? |
|
Definition
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Term
| What is the main therapeutic use of Beta1 Antagonist? |
|
Definition
Antihypertensives
Anti-angina |
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Term
| What is the main therapeutic use of Beta2 Agonist? |
|
Definition
| Relax bronchial smooth muscle |
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|
Term
| What is the main therapeutic use of Alpha2 Agonist? |
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Definition
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Term
| Where is Epinephrine produced? |
|
Definition
Adrenal Medullar
Hypothalamus
Brainstem |
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|
Term
| What does Epinephrine activate? |
|
Definition
Alpha 1 and 2
Beta 1 and 2 |
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Term
| T/F: Epinenphrine is inactive orally. |
|
Definition
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Term
| How does Epinephrine affect the heart? |
|
Definition
Increases contractility
Increases HR
Increase rate of relaxation |
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Term
| What metabolic effects does Epinephrine have? |
|
Definition
Increases glycogenolysis
Increase Lipolysis
Decreases insulin release
Increase metabolic rate |
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Term
| What are Epi effects on the Respiratory system? |
|
Definition
Relaxes the Bronchi via B2R
Stabilizes mast cell |
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Term
| What is EPI effect in the smooth muscles? |
|
Definition
Alpha1R causes sphincters to constrict
B2R cause peristalsis to decrease
B2R causes uterine smooth muscle to relax |
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Term
| The intra-ocular pressure is _______________ with EPI. It can also cause ______________. |
|
Definition
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Term
| List the therapeutic uses of EPI: |
|
Definition
1. Anaphylactic Shock
2. Prolong local Anesthetics (constricts the blood vessels to keep at the site)
3. Cardiac Stimulant
4. Bronchial asthma
5. Gluacoma ( decreaes the IOP) |
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Term
| What are some possible side effects of EPI? |
|
Definition
1. Tachycardia, arrhythmias
2. Elevated Blood Pressure
3. Tremors, restlessness, palpitations
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|
|
Term
| EPI is contraindicated with what? |
|
Definition
1. Peeps with Hyperthyroidism
2. Peeps taking selective B1 antagonist |
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|
Term
| What drug interactions occur with EPI and anesthetics? |
|
Definition
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Term
| What drug interactions occur btwn EPI and TCA, Cocaine and MAOi? |
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Definition
| Exaggerated response of EPI will occur. There will be more catecholamines in vesicles and synapes. The reuptake is blcoked so will ahve more Epi in the synapse. |
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Term
|
Definition
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Term
| What cardiac effects does NE have? |
|
Definition
1. Increases cardiac output
2. Decreases HR via Baroreceptor reflex |
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|
Term
| What side effects occur with NE ? |
|
Definition
1. Excessive vasoconstriction
2. Increased capillary filtration |
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Term
| Isoproterenol is only ____________, nonselective. |
|
Definition
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|
Term
| What effects does ISO have on the heart? |
|
Definition
Ionotropic and Chronotropic
(increases force and rate) |
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Term
| ISO is a vaso_________ and a broncho_______. |
|
Definition
Vasodilator (decreases TPR)
Bronchodilator |
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|
Term
| ISO is rapidly metabolized by ____________. |
|
Definition
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|
Term
| List the therapeutic uses for ISO. |
|
Definition
1. Cardiac arrest
2. Cardiogenic shock
3. Bronchodilation |
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|
Term
| Possible side effects of ISO include |
|
Definition
1. Tachycardia/arrhythmias
2. Palpitations, headache, flushing
3. Cardiac Ischemia |
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|
Term
| What receptors does DA act on? |
|
Definition
D1 and D2
B1 and B2
Alpha1 |
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Term
| DA has ionotropic and chronotropic affects on the heart. What effect does it have in the kidney? |
|
Definition
| It dilates the renal mesenteric arteries to maintain B.P. |
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Term
| Which receptors does Ephedrine/psuedophedrine stimulate? What does it cause the release of? |
|
Definition
|
|
Term
| What effects does Ephedrine/Psuedo have? |
|
Definition
1. Tachyphylaxis
2. Weight loss
3. Nasal Decongestant
4. Stimulant actions
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Term
| _______________ is a central and peripheral stimulant. |
|
Definition
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Term
| What are the therapeutic uses for amphetamines? |
|
Definition
1. Decreases food intake to aid in weihgt loss
2. Increases attention (high doses for Adderall)
3. Narcolepsy
4. Stimulant |
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Term
| Which isomer is the most potent for Amphetamine? |
|
Definition
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Term
| Phenylephrine is a selective ____________. |
|
Definition
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|
Term
| Which dosage form is the most potent for Phenlyephrine? |
|
Definition
|
|
Term
| T/F: Phenylephrine is a substrate for COMT |
|
Definition
| False; it is not a substrate. |
|
|
Term
| List the therapeutic uses for Phenylephrine |
|
Definition
1. Vasoconstriction
2. Decongestant
3. Mydriasis
4. Reflex dependent bradycardia |
|
|
Term
| Side effects of Phenylephrine include |
|
Definition
1. Excessive vasoconstriction
2. Rebound hyperemia
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|
Term
| Visine and Afrin both are____________ |
|
Definition
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