Block2Week1: Pharmacology

Front 1

What kind of ligand and receptors are used in the heart in the Sympathetic nervous system? What happens to HR?

Back 1

Norepinepherine binds to B1 (adrenergic) receptors in the heart. It innervates the SA and AV nodes increasing their conduction velocity, the contractility and heart rate.

Front 2

Give me the molecular biology involved for sympathetic innervation of the heart.

Back 2

The sympathetic nervous system acts through G(s) coupled receptors. The activation of these G-coupled protein receptors increases [CAMP] eliciting the increase of Na+ through "funny" receptors = faster depolarization.

Front 3

What kind of ligand and receptors are used in the heart in the Parasympathetic nervous system? What happens to HR?

Back 3

Ach binds to muscarinic receptors in the heart. Ach is released by the vagus nerve which innervates the SA node. This decreases your heart rate.

Front 4

Give me the molecular biology involved for parasympathetic innervation of the heart.

Back 4

The parasympathetic nervous system acts through G(i) couple receptors. Their activation decreases [CAMP] and directly opens K+ channels = slower depolarization.

Front 5

You are running through the forrest and you see a pack of wolves. What happens to your body?

Back 5

Your sympathetic nervous system kicks in: dilation of pupils, decrease in gastric motility, increase of your heart rate and an increase in your blood pressure.

Front 6

After you run away from the wolves, you rest by leaning on a pine tree. What is happening to your body?

Back 6

With an increase of BP, your baroreceptors signal your cardiovascular control center (PANS) to decrease your heart rate (wants to go back to homeostatis). This is done through the vagus nerve. There is vasodilation of your blood vessels and their is a decrease of contraction of your heart = decreasing your BP.

Front 7

What happens if you increase your total peripheral resistance (TPR)?

Back 7

This will increase your BP through alpha-1 resulting in vasoconstriction of your blood vessels. This will decrease your HR = reflex bradycardia.

Front 8

What happens if you decrease your total peripheral resistance (TPR)?

Back 8

This will decrease your BP through B2 or Muscarinic stimulation resulting in vasodilation of your blood vessels. The result will increase your HR = reflex tachycardia.

Front 9

You give Norepi to your patients what happens to their BP and heart rate?

Back 9

Norepi will increase the BP and decrease the HR of the patient.

Front 10

What are the binding efficiencies of receptors for Norepi?

Back 10

Alpha and B1 effects at low concentrations and at higher concentrations, B2.

Front 11

What happens to the BP and HR when you block Norepi alpha receptors?

Back 11

There is a small rise of BP and an increase of HR. This unmasks the Beta receptors.

Front 12

What happens to BP and HR when you block Norepi beta receptors?

Back 12

There is an increase of BP with a decrease of HR.

Front 13

If you bind alpha-1 receptors what happens?

Back 13

The binding of Norepi to alpha-1 receptors constricts blood vessels = reflex bradycardia.

Front 14

What are the binding efficiencies for Epi?

Back 14

Beta 1 and B2 effects at low concentrations and at higher concentrations, alpha.

Front 15

What are the differences between Norepi and Epi in comparison to HR and BP?

Back 15

Epi shows a biphasic curve. At [low], there is an increase of BP and a decrease of HR. At [higher] there is a decrease of BP and an increase of HR.

Front 16

You block Epi alpha receptors, what happens to the HR and BP?

Back 16

There is a decrease in BP and an increase of HR.

Front 17

If you block Epi beta receptors, what happens to the HR and BP?

Back 17

There is an increase of BP and a decrease of HR.

Front 18

Name two enzymes that degrade Ach. Give their locations.

Back 18

Acetylcholinesterase: found in synapses and erythrocytes.

Butrylcholinesterase/plasma cholinesterase: found in the serum and liver, is a scavenging enzyme for all drugs.

Front 19

You give Ach to your patient what happens to their BP and HR?

Back 19

At [low] of Ach, there is a decrease of BP and an small increase of HR. At [higher], there is a large decrease of BP resulting in direct bradycardia then a reflex tachycardia. Later on, there is Ach release from the adrenal medula.

Front 20

What receptors are in excess in the lungs? What happens if you block these receptors?

Back 20

Beta receptors are in excess. Sympathetics will act on these receptors, relaxing the bronchioles and decreasing secretions. Blocking these receptors will result in vasoconstriction and an increase of secretions.

Front 21

What are the major functions of the Sympathetic Nervous system?

Back 21

Increase CO, increase blood flow to needed organs, decrease of blood flow to non-essential organs, decrease GI and urinary activity, increase of blood glucose

Front 22

What kind of drugs mimic the Sympathetic Nervous system?

Back 22

Sympathomimetics

Front 23

What kind of drugs inhibit the Sympathetic Nervous system?

Back 23

Sympatholytics

Front 24

What are the sites of action of sympathomimetics?

Back 24

Indirect acting: Releasing agents, MAOIs, Reuptake inhibitors, alpha blockers.

Direct acting: Catecholamines, non-catecholamines

Front 25

What are the affects of sympathomimetics on smooth muscle?

Back 25

Bronchial smooth muscle (primarily beta receptors) relax

Heart: increase force of contraction, stroke volume and cardiac output increases, an increase of arrhythmias, an increase of oxygen consumption.

Front 26

Where are B receptors found?

Back 26

Blood vessels of visceral organs (kidney and skeletal muscles) contain beta receptors. In addition, beta receptors are in excess in the lung.

Front 27

What do alpha agonists do? Name an alpha agonist drug.

Back 27

Vasoconstriction, causing a reflex bradycardia. Phenylephrine.

Front 28

What do B1 agonist do? Name a B1 agonist drug.

Back 28

Increase force and rate of contraction of the heart. Dobutamine.

Front 29

What do B2 agonist do? Name B2 agonist drugs.

Back 29

The major affect of B2 agonist is a decrease of blood pressure and bronchodilatation. Terbutaline and albuterol.

Front 30

What are the affects of Norepi?

Back 30

Norepi decreases the pulse rate and increasing the blood pressure. The peripheral resistance therefore is increased. Norepi binds to alpha receptors at [low] and binds to beta receptors at [high].

Front 31

What are the affects of Epi?

Back 31

There is an increase of heart rate and a decrease of blood pressure. The peripheral resistance therefore is decreased. Epi binds to beta receptors at [low] and to alpha receptors at [high].

Front 32

What are the affects of Isoproterenol?

Back 32

There is a substantial increase of heart rate and a decrease of blood pressure. There is a substantial decrease of peripheral resistance.

Front 33

Name sympathomimetic drugs and their actions.

Back 33

Amphetamine: taken up by presynaptic nerve terminals, displacing NE, EPI from storage sites. They mimic NE and EPI.

Pargyline and Tranylcypromine (MAO inhibitors): enhance NE and EPI effects.

Cocaine, Tricyclic antidepressants (reuptake inhibitors): exaggerate adrenergic responses.

Yohimibine (alpha blockers): enhanced sympathetic activity.

Front 34

Name sympatholytic agents and their actions.

Back 34

Alpha-blocker (phentolamine), Beta-blocker (propranolol): inhibit ability of neurotransmitter.

Clonidine (alpha 2 agonist): decrease CNS sympathetic outfow.

Reserpine: interfere with the synthesis and release of NE.

Front 35

What are the side effects of sympatholytic agents?

Back 35

Increases blood volume and Na+ retention (decreasing glomerular filtration), sedation and depression.

Front 36

What are the side effects of alpha blockers?

Back 36

Nasal stuffiness and increase of GI motility and diarrhea. Postural hypotenision (reflex tachycardia)and impaired ejaculation.

Front 37

What are the side effects of the beta-adrenergic blocker?

Back 37

Bradycardia, decrease of cardiac output which may lead to CHF, effect sensitivity to insulin and oral hypoglycemics, bonchoconstriction, increase of TAGS, and decrease of CO (cold extremities).

Front 38

What are the actions of beta blockers?

Back 38

A decrease of HR, contractility, CO, conduction velocity of the heart, AV conduction, and cardiac work.

In addition, there is a decrease of renin, glycogenolysis activity, and lipolytic activity./

Front 39

What are the effects of muscarinic agonists (cholinomimetics, parsympathomimetics)?

Back 39

Bradycardia, vasodilation via muscarinic receptors in the blood vessels leading to an indirect tachycardia, increased secretions of fluids, bronchoconstriction, increase peristaltic activity, and pupillary constriction.

Front 40

What is dysautonomia? How do you test for this disease?

Back 40

It is a rare recessively inherited disease that is characterized by small fiber peripheral neuropathy. To test for this you give METHALCHOLINE = their pupil constrict. Since these patients have less fibers, a small amount will elicit an effect.

Front 41

Name the 3 classes of Cholinesterase inhibitors. Give me drug examples for each.

Back 41

1) Revesible competitive (very short) (EDROPHONIUM)
2) Carbamate inhibitior (short duration) (NEOSTIGMINE)
3) Phosphonate (irrevesible inhibitor, lifetime of enzyme) (DFP)

Cholineestarase inhibitors bloks all preganglions.

Front 42

Where are nicotinic receptors are? Where are muscarinic receptors?

Back 42

Nicotinic receptors are found preganglionic in both sympathetic and parasympathetics. Muscarinic receptors are found post ganglionic.

Front 43

Name Antimuscarinic (anticholinergic) agents. What are their side effects.

Back 43

Atropine, Methlatropine, Ipratropium.

You have an increase of HR, reduced sweating, dry mouth, reduced GI and bladder motility, reduced bronchial mucous secretion and dilation of bronchioles, and sedation of CNS.

Front 44

Name a Ganglionic nicotinic receptor blocking agent.

Back 44

Trimethaphan: a short acting ganglionic blocking agent infused via IV during surgery.

Front 45

What are the effect of Ganglionic nicotinic receptor blockers?

Back 45

Vasodilation, failure of sweat glands, tachycardia, dilated pupils, decreased GI tract tone, urinary retention, and dry mouth.