Ans Pharmacology

Front 1

6 categories of cholinergic drugs

Back 1

1. Ganglionic stimulating agents

2. Ganglionic (nicotinic receptors)

3. Muscarinic Agonist

4. Cholinesterase inhibitors

5. Muscarinic antagonist

6. Neuromuscular Blocking agents

Front 2

Nicotine

Back 2

Mimics ACh at nicotinic receptors on autonomic ganglia

-little to use

- side eff, (inc BP, Withdrawal)

Front 3

Ganglionic (nicotinic receptors) blocking agents

Back 3

*Hexamethonium

-1st drug developed for HTN treatment

* Mecamylamine (invesine)

* Trimethaphan (Afronad)

*** DIRTY DRUGS***

Front 4

What medication was 1st used to treat HTN

Back 4

Hexamethonium

Front 5

What is the use for ganglionic blocking agents?

Back 5

* block nicotinic receptors at sympathetic auto ganglia

* have low selectivity and large amount of effects

* used in experiments to prevent Vagal reflexes to change blood pressure ***used to prevent reflex Brady cardia caused from Nor Epi

Front 6

What is an important way Ganglionic blocking agents have been used experimentally?

Back 6

Have been used to prevent vagal reflexes responses to blood pressure such as to prevent Bradycardia caused by NE

Front 7

Toxicity of Ganglionic Nicotinic receptor blockers

Back 7

*Severe orthostatic hypertension

* Cycloplegia w loss of accommodation

* constipation

* sexual dysfunction (erection/ejaculation)

Front 8

Ganglionic nicotinic receptor blocking agents inverse reactions

Back 8

Whenever you block nicotinic receptors of the sympathetic division, you will also stimulate parasympathetic functions

** remember these are all non selective so they bind to all kinds of stuff ***

Front 9

Commonly used Ganglionic nicotinic receptor blocking agents

Back 9

*Buproprion (Wellbutrin)

-antidepressant

* Dexatromethorphan

-cough suppressant

Front 10

What class of drugs does buproprion (Wellbutrin) fall under and what is it used for?

Back 10

Buproprion (Wellbutrin) is a Ganglionic receptor blocking agent and this used as an Anti-Depressant

Front 11

What class of drug is Dextromethorphan under and what is it used for?

Back 11

Dextromethorphan is a ganglionic nicotinic receptor blocker that is used as a Cough Supressant

Front 12

MOA for Dextromethorphan

Back 12

N-Methyl-D-Aspartate (NDMA) receptor antagonist, seratonin reuptake inhibitor

Front 13

MOA for Buproprion (Wellbutrin)

Back 13

Norepinephrine-dopamine reuptake inhibitor

Front 14

What is the mechanism of action of Wellbutrin?

Back 14

Norepinephrine- Dopamine reuptake inhibitor

**remember this is a antidepressant so you want to increase the amount of norepinephrine and dopamine in the system

Front 15

What is a major disadvantage of using Buproprion/Dextromethorphan?

Back 15

Increase the risk of Angle Closure Glaucoma

Front 16

Muscarinic agonist

Back 16

Two types

* Esters

* Alkaloids

Front 17

Bethanechol and Pilocarpine are in which category of Cholinergic drugs?

Back 17

Muscarinic Agonist

Front 18

Clinical uses for Bethanechol and Pilocarpine?

Back 18

Tx of acute angle closure glaucoma and open angle glaucoma

(These are non selective activation of Muscarinic receptors)

Front 19

Treatment uses for Muscarinic agonist

Back 19

Urinary retention

Dry mouth

Glaucoma (acute angle closure glaucoma a open angle glaucoma)

Front 20

What does Pilocarpine do?

Back 20

It contracts the colliery muscle and opens up the trabecular mess work for aqueous outflow

**Miosis**

Front 21

What is the mechanism of action of Duvoid and PiloCarpine?

Back 21

Binds to Muscarinic receptors and activates

Front 22

Bethanechol uses

Back 22

urinary retention, dry mouth and glaucoma

Front 23

When do you use Pilocarpine?

Back 23

Whenever the IOP is less than 40

Front 24

Cholinergic toxicity

Back 24

DUMBELS

D-diarrhea

U-Urination

M-Miosis

B-Bronchoconstriction

E- Exitation of skel muscles and CNS

L- Lacrimation

S- Salvation/ sweating

Front 25

Cholinergic Regenerators

Back 25

Reactivates Cholinesterase and reactivates it

Used when body has too much ACh and needs to remove it (DUMBEL)

Front 26

Cholinergic Regenerators

Back 26

Pralidoxime (Protopam)

-for nerve gas poisoning

With poisoning there’s no side effects from treatment

Front 27

Muscarinic Antagonist

Back 27

Atropine

-Competitive non-Selective Non-specific Muscarinic blocker

Scopolamine

-prevents motion sickness

-patch

Front 28

Atropine

Back 28

Competitive non-specific non-selective Muscarinic blocker

“Binds to Muscarinic receptors but doesn’t activate them

Front 29

Theraputic uses for Atropine

Back 29

Eye- mydriatic, cycloplegia, myopia control

Heart- Anti-arrhythmia (bradycardia)

Secretions- hyperhidosis,rhinitis

Poisoning- Organophosphates

***remember Atropine is a Muscarinic antagonist so its trying to stop AChesterase inhibitors***

Front 30

Which one of these is not a use for Atropine

Back 30

-Brady Cardia

- Cycloplegia

- Organophosphate poisoning

- Rhinitis

**all are uses for Atropine**

Front 31

H

Back 31

h

Front 32

What are some side effects of PiloCarpine

Back 32

Vasodilation-leads to hypotension

Excessive salivation, increase gastric acid output

Contraindications- Hyperthyroidism - body responds to hypotension by releasing NorEpi

Front 33

ACh esterase inhibitors

Back 33

2 groups

Reversible-non CNS/CNS

Irreversible-no Thera relevance

MOA- binds to Enzyme that degrades ACh and inhibits it

Front 34

Neostigmine(Prostigmin)

Edrophonium (Enlon)

Physostigmine (Eserine)

Back 34

All AChesterase inhibitors

Does the same thing as agonist but has a different rout

Front 35

NeoStigmine, Edrophonium and Physostigmine are all under which type of drug?

Back 35

AChesteras inhibitors

Front 36

Therapeutic uses for AChesterase inhibitors

Back 36

*Myasthenia Gravis

* reversal of competitive neuromuscular blockage

*Atropine poisoning

-reduces ACh

Front 37

Myasthenia Gravis

Back 37

Autoimmune disorder that attacks muscle causing weakness and fatigue (attacks AChr)

First sx can be

-weekness of eye muscles, difficulty swallowing and slurred speech

Front 38

ACh esterase inhibitors that cross BBB

Back 38

Rivastigmine (Exelon)

Doneprezil (Aricept)

Front 39

Rivastigmine and Doneprezil have what MOA and tx use?

Back 39

They are AChesterase inhibitors that cross the BBB.

Tx- Alzheimer’s (doesn’t cure but slows it down)

Front 40

Irreversible Cholinesterase inhibitors

Back 40

No Tx usefulness

-Organophosphates (esters and Phoric Acid)

-highly toxic