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Pharm Unit 1 > 3. Pharmacologic Cholinergics > Flashcards

3. Pharmacologic Cholinergics Flashcards

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1
Q

Drugs with what type of ganglionic target effects all autonomic functions? What is the end result?

A

Nicotinic (cuz all have preganglionic nicotinic receptor)

The dominant tone in every organ is antagonized

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2
Q

Autonomic drugs can target what different regions?

A

CNS Acting (signal origin)
Ganglion blockers
(Postganglionic) Neuron blocker
(Distal) Receptor Blocker

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3
Q

What toxin blocks Ach release? What organ can it not effect? Why?

A

Botulinum toxin

Can’t reach brain because it is a protein

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4
Q

What are the pharmacologic nicotinic ganglionic receptor agonists? Effects? Clinical uses?

A

Only Nicotine
Receptor stimulation then depression + CNS stimulant (cause of addiction)
Treatment of nicotine withdrawal (oral or transdermal)

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5
Q

What are the pharmacologic nicotinic ganglionic receptor antagonists?

A

Hexomethonium
Mecamylamine
Trimethapham

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6
Q

Which ganglionic receptor antagonists can penetrate into CNS? Which one can’t?

A

Mecamylamine

Hexomethonium

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7
Q

What is the treatment of choice for a patient that presents with convulsions due to nicotine overdose?

A

Mecamylamine (cuz can get into CNS)

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8
Q

What was a previous use for ganglionic receptor antagonists that is no longer indicated due to the high level of side effects?

A

Hypertension treatment

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9
Q

Effect of ganglionic receptor antagonists on arterioles & veins?

A

Decrease in symp –> hypotension, postural hypotension & decreased CO

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10
Q

Effect of ganglionic receptor antagonists on the heart?

A

decreased para –> increased HR = tachycardia

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11
Q

Effect of ganglionic receptor antagonists on the Iris?

A

decreased para –> pupil dilation = mydriasis

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12
Q

Effect of ganglionic receptor antagonists on the ciliary muscle?

A

decreased para –> loss of accomodation = cyclopegia

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13
Q

Effect of ganglionic receptor antagonists on GI system?

A

decreased para –> less tone = constipation

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14
Q

Effect of ganglionic receptor antagonists on the bladder?

A

decreased para –> urinary retention

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15
Q

Effect of ganglionic receptor antagonists on salivary gland?

A

decreased para –> dry mouth = xerostomia

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16
Q

Effect of ganglionic receptor antagonists on sweat glands?

A

decreased symp –> decreased ability to thermo regulate = hypothermia

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17
Q

What are the pharmacologic muscarin agonists?

A

Choline esters = acetylcholine, methacholine & bethanechol

Alkaloids = muscarine & pilocarpine

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18
Q

In terms of pharmacologic action, what is acetlycholine? Clinical uses?

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A

Muscarinic agonist

Only eye surgery

19
Q

In terms of pharmacologic action, what is methacholine? Clinical uses?

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A

Muscarinic agonist

Test bronchial reactivity

20
Q

In terms of pharmacologic action, what is Bethanechol? Clincial uses?

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A

Muscarinic agonist

increase urination

21
Q

Which pharmacologic muscarinic agonist is metabolized rapidly? Slowly? Not metabolized?

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A

Acetylcholine
Methacholine
Bethanechol

22
Q

In terms of pharmacologic action, what is pilocarpine? Clinical uses?

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A

Muscarinic agonist

Treat glaucoma or increase salivation

23
Q

What is the “historical” muscarinic antagonist & its use?

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A

Belladona
Used to cause pupil dilation
Long acting

24
Q

In high doses, antimuscarinics can cause what CNS signs?

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A

Hallucinations

25
"Current" protoype antimuscarinic drugs?
Atropine | Scopalamine
26
Clinical uses of antimuscarinic drugs?
Decrease tremors in parkinsons Treat motion sickness Inhibit salivation during oral surgery Treat insecticide poisoning (decrease effects of anticholinesterases) MI treatment (blocks vagal response to pain so HR can increase) Asthma Pupil dilation during eye examination
27
In terms of pharmacologic action, what is Ipratropium? Clinical uses?
Muscarinic antagonist Asthma treatment, inhaled as charged molecules which stay in lung
28
What is the physiologic effect of cholinesterase inhibitors?
prolong acetylcholine action at synpase --> like giving acetylcholine Instead of binding once, can bind up to 5 times before being degraded
29
What are the clinical uses of reversible cholinesterase inhibitors?
Myastenia gravis (autoimmune loss of Ach receptors) Glaucoma Alzhiemers Reversal of nueromuscular block after surgery
30
What are the therapeutic anti-cholinesterases?
Class name = carbamate ``` Physostigmine Neostigmine Edrophonium Donezepil Galantanine ```
31
What are the main 2 anti-cholinesterases & the main difference between them?
Physostimine, uncharged & enters CNS | Neostigmine, charged & doesn't enter CNS
32
What is the short acting anti-cholinesterase used for used for testing myastinea gravis?
Edrophonium
33
What anti-cholinesterases are used to treat alzhiemers? Safety & efficacy?
Donezepil & Galantanine | Don't harm, not very effective
34
What are the clinical uses of irreversible anti-cholinergics?
There are none It is used as insecticides & nerve gas
35
In terms of pharmacologic action, what is diisopropylfluorophosphate (DFP)? Clinical uses?
Irreversible anti-colinesterase Insecticides & nerve gas
36
What are organophosphates?
Irreversible anti-colinesterase
37
Who is suseptible to organophosphate poisoning? Treatment?
Young children in rural areas (near farms) & military Atropine & pralidoxime
38
How do organophasphates work?
Aging = slow process where organophosphate-cholinesterase complex becomes covalenty & irreversibly bound
39
In terms of pharmacologic action, what is Atropine? Clinical uses?
Muscarinic receptor blocker used for organophsophate poisoning. Targets brain where seizures can be life threatening
40
In terms of pharmacologic action, what is Pralidoxime? Clinical uses?
Used for organophosphate poisoning, binds the poison & removes it if aging process hasn't had time to occur. Does not cross BBB
41
What is a disease (not addiction) that can be treated with nicotinic agonist? Why does it work?
Alzhiemers | Cholinergic neurons are most susceptible during alzhiemers --> less Ach
42
What does muscarinic receptor activation lead to?
Ion channels opening, kinases, phosphatases, protease, gene regulation Ca, IP3, cAMP, cGMP
43
Which nicotinic ganglionic antagonist is used in neurosurgery?
trimethapram

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