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58 Cards in this Set

  • Front
  • Back

What are the two classifications of Sympathomimetics? Describe them

1. Direct- works directly with the receptors


2. Indirect- Dependant on the release of Catecholamines

What are the 2 type of Indirect Sympathomimetic drugs

1. They diplace the Catecholamines from the free nerve endings


2. Inhibit their reuptake so they can stay in the synapse longer.

What are some examples of Indirect Sympathomimetic drugs that diplace Catecholamines?

Amphetamine and Tyramine

What are some examples of indirect Sympathomimetics that inhibit the reuptake of Catecholamines?

Cocaine and Tricyclic Antidepressants

What is the relationship between Side groups and selectivity of Catecholamines?

The larger the group the more selective it is! w

Which Catecholamine is the most selective?

Isoproterenol

Which adrenoreceptor increases Arterial Resitance and BP?

Alpha 1


Which Adrenoreceptor promotes smooth muslce relacation and decreases Arterial resistance?

Beta 1?

The skin and Splancchine vessels have predominatly what type of receptors?



What do they do in they do int he prescence of NE and Epi?

Alpha 1 they Constrict

What receptors must be on skeletal muscle in order for them to dialate?

Beta Receptors

Direct effects on the heart are determined largely by what type of receptors?



What does it cause?


Beta 1 Influx of Calcium thus it increases HR and FOC!

Beta 3 Receptors?

Increases Lipolysis


Alpha 2 receptors _________ Insulin secretion?

Decrease


Beta Receptors _______ Insuline Secretion

Increase

What do Alpha-1 agonist do the BP?

Increase TPR, Increase BP.


What is an example of an Alpha-1 Agonist that INCREASES BP

Phenylephrine

Beta 1 on BP???

Increases HR, Increase FOC, Increases BP


Beta 2 on BP?

Decrease TPR via VASODILATION, in certain vascular beds


Isoproterenol on BP

Increase CO but Dec TPR by activating B2 receptors

The importance of Amphetamine on the CNS?

Catecholamines do not enter the CNS effectively. AMPH can enter the CNS and will thus cause Stiumulant effects

Amphetamine

Increases allertness, Reduces fatigue, anorexia, Euphoria and insomina?


Very high does of Amphetamine will result in?

agressiveness, marked anxiety and convulsionA

Alpha receptors on they eye. Give a drug example

causes dilation. Phenylephrine

Alpha-2 selective agonist that increase the decrease aqueous solution

Apraclonidine and Brimonidine

Beta Antagonist drug that is used in Glaucoma. What is its Mechanism?

Timolol. Decreases the production of Aqueous humor!

What type of receptors cause nasal decongestion?

Alpha 2

Why would you use Beta 2 receptors in Bronchial Asthma?

It causes bronchial dilation by smooth muscle relaxation.

Beta 2 receptors on the uterus. What are they useful for?

Beta 2 receptors cause smooth muscle relaxation of the uterues and can be used for premature labor.

IMPORTANT!!!! What is located on the base of the bladder, urethral sphincter and prostate? What do they do?


alpha 1 subtype-A- receptors. they mediate contraction and can thus promote urinary contienence!

What will beta 2 receptors on the bladder mediate?

Smooth muscle relaxation

What do alpha receptors in the ductus deferens, seminal vescicles and prostate help in?

Ejaculation.

Beta 1 _______ renin secretion

increase

What are the actions of Epinephrine? On the heart and bv?

Vasocontrictor and Cardiac stimulant. Alpha 1 is on the blood vessels and causes vasoconstriction. Beta 1 is on the heart and increases Hr.


What is the effect of Epinephrine with Beta-2 receptors

They are located on skeletal muscle blood vessels and will cause vasodilation. causes TPR to fall and contributes to increased blood flow during exercise

What are the effects of Epi in high does versus low doses?

High does- Alpha 1 and Beta 1


Low doese- Beta receptors only! - increase HR and Decrease BP!

What is the receptor selectivity of Beta receptors on NE?

Alpha 1 = Alpha 2 Beta 1 and VERY LITTLE Beta 2

Explain the baroreflex activation

Increases BP and Decreases HR

What are the positive inotropic effects of NE?

Increase FOC and contractility

Isopreoterenol

Potent B-receptors and little effect on Alpha receptors.

Isoproterenol is selective to which receptor?

Beta 2- good vasodialator with increased CO and a fall in diastolic and mean arterial pressure.

What type of receptors does dopamine activate?

D1-Vasodilation in kidneys


Low doses of Dopamine?


High doses of Dopamine?

Low- 2-5 mcg/kg/min acts on Dopaminergic receptors and causes renal, coronary and cerebral blood flow.


above 5- Beta receptors and increases release of NE- Increased cardiac contractablity.


10-20- Alpha receptors-vasoconstriction

Dobutamine

B1 selective synthetic catercholamine

Amphetamine IMPORTANT

Can enter CNS and is a displacer. increases mood and alertness and depresses appetite

Methamphetamine-IMPORTANT

similar to amphetamine but with higher ration of central to peripheral actions

Dextroamphetamine (Adderall)-IMPORTANT

another CNS stimulant that is used for concentration

Cocaine

Reuptake inhibitor of Dopamine. (pleasure centers)


has an amphertamine like effect but is short acting but MORE INTESNSE.


Ephedrine

Mixed acting Sympathomimetics


found in plants


access ot CNS and is a mild stimulant


displaces NE from the presynaptice Neurons

What are mixed acting Sympathomimetics?

are both direct and indirect aympathomimetics

Psuedo ephedrine

over the counter


in decongestants

Alpha Agonist

Phenylephrine, Xylometrazoline and Oxymetazoline

Phenylephrine

Alpha 1 agonist


decongestant and mydriatic

Xylometazoline and oxymetazoline

preferred nasal decongestant


alpha agonist


nasal constriction of the nasal mucosa

Alpha 2 agonist

Clonidine, Methlydopa


Clonodine and Methlydopa

used for HTN, narcotic addicts and diazapam withdrawals


Side effects of Clonidine and Methlydopa

Postural hypotension, dry mouth, sedation and rebound htn


Apraclonidine

Clonidine derivative used in glaucoma!


Tyramine

by product of tyrosine metabolism


found in cheese


indirect effect to relesase of catecholamines


similar to NE


TAKING MAOI inhibitors you should avoid tyramine foods