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Colin CPR II > Drugs > Flashcards

Drugs Flashcards

1
Q

What protein is associated with Nicotinic ACh Receptors?

A

Na+/K+ Depolarizing Ion Channel

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2
Q

Where are Nicotinic M ACh Receptors located?

A

Skeletal Muscle Neuromuscular Junction

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3
Q

Where are Nicotinic N ACh Receptors located?

A
  • Ganglia (post-ganglionic cell body)
  • Dendrites
    CNS
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4
Q

What protein is associated with M1 ACh Receptors?

A

Gq GPCR

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5
Q

What protein is associated with M2 ACh Receptors?

A

Gi GPCR

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6
Q

What protein is associated with M3 ACh Receptors?

A

Gq GPCR

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7
Q

What is the MOA of Gq GPCR?

A

PIP2 –> IP3/DAG –> Increase intracellular Ca2+

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8
Q

What is the MOA of Gs GPCR?

A

Increase cAMP

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9
Q

What is the MOA of Gi GPCR?

A

Decrease cAMP

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10
Q

Where are M1 ACh Receptors located?

A
  • CNS

- Enteric NS

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11
Q

Where are M2 ACh Receptors located?

A
  • Atria
  • SA node
  • AV node
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12
Q

Where are M3 ACh Receptors located?

A
  • Glands (including sweat)
  • Bladder (detrusor, sphincter)
  • Lungs
  • Smooth Muscle (including endothelium and eye)
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13
Q

What protein is associated with M4 ACh Receptors?

A

Gi GPCR

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14
Q

What protein is associated with M5 ACh Receptors?

A

Gq GPCR

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15
Q

Where are M4 ACh Receptors located?

A

CNS

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16
Q

Where are M5 ACh Receptors located?

A

CNS

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17
Q

What is Bethanechol?

A

Direct Cholinomimetic Drug (Muscarinic Agonist)

Interacts with MAChRs

Used to treat Non-obstructive GI Dysmotility (Post-op Ileus, Neurogenic Ileus, Congenital Megacolon)
- Causes GI motility

Used to treat Urinary Retention
- Causes Detrusor muscle (bladder) activation and urinary sphincter relaxation

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18
Q

What is Atropine?

A

Muscarinic Antagonist

Non-selective M1 = M2 = M3

Used to treat Cholinergic Poisoning when used with Pralidoxime
- Blocks MAChRs from interacting with ACh or other agonists

Used to block vagal reflexes induced by surgical maniulation

Used to treat GI disorders
- Inhibits GI motility

Used to treat bradycardia

Used to treat heart block

Tertiary Agent - CAN cross the BBB

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19
Q

What is Pralidoxime?

A

ACh Esterase Regenerator

Used with Atropine to reverse Cholinergic Poisoning (too much ACh or ACh agonists)

Pralidoxime acts peripherally, not centrally

CANNOT cross the BBB

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20
Q

What is Carbachol?

A

Direct Cholinomimetic Drug - Nicotinic and Muscarinic Agonist

Interacts with Muscarinic and Nicotinic ACh Receptors

Used to treat acute angle glaucoma

  • Causes Ciliary Muscle contraction - outflow of aqueous humor
  • Causes Pupillary muscle constriction (miosis)
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21
Q

What is Tacrine?

A

Indirect Cholinomimetic Drug - Acetylcholinesterase Inhibitor

Binds to AChE

Tertiary Agent - CAN cross the BBB

Used to treat Alzheimer’s Type Dementia

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22
Q

What is Cevimeline?

A

Direct Cholinomimetic Drug

Used as an oral tablet to treat xerostomia (dry mouth) in patients with Sjogrens Syndrome

Metabolzied by P450 pathways and eliminated in urine

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23
Q

What is Rivastigmine?

A

Indirect Cholinomimetic Drug - Acetylcholinesterase Inhibitor

Tertiary Agent - CAN Cross the BBB

Used to treat Alzheimer’s Type Dementia

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24
Q

What is Methacholine?

A

Direct Cholinomimetic Drug

Causes bronchial smooth muscle contraction

Used for pulmonary testing - can exacerbate Asthma/COPD

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25
Q

What is Pyridostigmine?

A

Indirect Cholinomimetic Drug - Acetylcholinesterase Inhibitor

Carbamic Acid Ester (carbamate)

Quarternary Agent - CANNOT cross the BBB

Used to treat patients with Myasthenia Gravis

Out-competes Myasthenia Gravis Antibodies

Increases ACh in the Neuromuscular Junction endplate

26
Q

What is Pilocarpine?

A

Direct Cholinomimetic Drug - Muscarinic Agonist

Used to treat xerostomia (dry mouth) in patients with Sjogrens Syndrome or head and neck cancer related xerostomia

Causes several effects on the eye:

  • Causes contraction of Pupillary muscles (miosis contraction of pupil)
  • Causes contraction of the Ciliary muscles (accommodation of the lens - more round for near site)
  • Causes outflow of aqueous humor, reducing occular pressure

Used to treat glaucoma

27
Q

What is Physostigmine?

A

Indirect Cholinomimetic Drug - Acetylcholinesterase Inhibitor

Binding to AChE is covalent and irreversible

Tertiary Agent - CAN cross the BBB

Used to reverse Atropine overdose (diminished cholinergic signaling - excessive sympathetic state) - peripheral and central effects

Used to treat Alzheimer’s Type Dementia

28
Q

What is Varenicline?

A

Direct Cholinomimetic Drug - Nicotinic Agonist

Interacts with Nicotinic ACh Receptors

Does NOT interact with MAChRs

Used only to help quite smoking

29
Q

What is Neostigmine?

A

Indirect Cholinomimetic Drug - Acetylcholinesterase Inhibitor

Carbamic Acid Ester (carbamate)

Binding to AChE is non-covalent and reversible

Used to treat Myasthenia Gravis

  • Outcompetes Myasthenia Gravis Antibodies
  • Increases ACh in the Neuromuscular Junction endplate

Used to reverse pharmacological paralysis induced by Neuromuscular Blocking drugs during surgical anesthesia

Quaternary Agent - CANNOT cross the BBB

30
Q

What is Abenonium?

A

Indirect Cholinomimetic Drug - Acetylcholinesterase Inhibitor

Quaternary Agent - CANNOT cross the BBB

31
Q

What is Scopolamine?

A

Muscarinic Antagonist

Used to treat motion sickness

Used in Ophthalmology

  • Causes mydriasis (pupil dilation)
  • Blocks cholinergic activation of Pupillary muscle constriction

CAN cross the BBB

Can be administered by injection, orally, or transdermal patch

32
Q

What is Donepezil?

A

Indirect Cholinomimetic Drug - Acetylcholinesterase Inhibitor

Used to treat Alzheimer’s Type Dementia

Tertiary Agent - CAN cross the BBB

33
Q

What is Ipratropium?

A

Muscarinic Antagonist

Specificity for M3 receptors

Used to treat respiratory disorders (COPD/Asthma)
- Block muscarinic activity, promoting sympathetics (Bronchodilation, reduced pulmonary secretions)

Dissociates from M3 faster than Tiotropium

Has shorter bronchodilator action

34
Q

What is Echothiphate?

A

Indirect cholinomimetic Drug - Acetylcholinesterase Inhibitor

Organophosphate

Binding to AChE is covalent and irreversible

Quaternary Agent - CANNOT cross the BBB

35
Q

What is Oxybutinin?

A

Muscarinic Agonist

Specificity for M3 receptors

Used to treat urinary disorders (overactive bladder)
- Relieves bladder spasms after urologic surgery

Relax smooth muscle in the ureters and bladder wall

Side effects:
o Dry mouth, dizziness, constipation, blurred vision, dry eyes, urinary tract infections

36
Q

What is Edrophonium?

A

Indirect Cholinomimetic Drug - Acetylcholinesterase Inhibitor

Alcohol; positively charged

Binding to AChE is non-covalent and reversible

Outcompetes MG Antibodies

Has short half-life, only effective for 5-10 min, thus not very effective MG treatment

Used for Tensilon Test

  • Reverses muscle weakness in undertreated MG patients (POSITIVE TENSILON TEST)
  • If it fails to reverse muscle weakness, then you have a NEGATIVE TENSILON TEST (this indicates patient is in Cholinergic Crisis; aka too much ACh or agonist)

Quaternary Agent - CANNOT cross the BBB

37
Q

What is Tiotropium?

A

Muscarinic Antagonist

Specificity for M3 receptor

Used to treat respiratory disorders (Asthma/COPD)

Blocks muscarinic activity, promoting sympathetics (Bronchodilation, reduced pulmonary secretions)

Dissociates from M3 receptor slower than Ipratropium
- Longer bronchodilator action

38
Q

What is Galantamine?

A

Indirect Cholinomimetic Drug - Acetylcholinesterase inhibitor

Used to treat Alzheimer’s Type Dementia

Tertiary Agent - CAN cross the BBB

39
Q

What is Tolterodine?

A

Muscarinic Antagonist

Used for urinary disorders (overactive bladder)
- Relieves adult urinary incontinence

40
Q

What is Benztropine?

A

Muscarinic Antagonist

Selectivity for M1

Centrally acting

Used for movement disorders (Parkinson’s Disease)

Treat tremor and rigidity in Parkinson’s
- Blocks excess cholinergic activity (excessive M1 activation is associated with cogwheel rigidity)

41
Q

What is Mecamylamine?

A

Ganglion Blocker

Competitively block action of ACh and similar agonists at NAChRs of both the parasympathetic and sympathetic autonomic ganglia
- Block all autonomic flow

CAN cross the BBB

Enhances sympathetic tone:

  • CNS: sedation, tremor, choreiform movements, and mental aberrations
  • Eye: Cycloplegia (paralysis of ciliary muscles; loss of accommodation; lens can’t be adjusted), Moderate dilation of pupil
  • Cardiovascular: Decreased blood pressure, diminished contractility, moderate tachycardia
  • GI: Reduced secretion, profound motility inhibition
  • GU: Urination hesitancy, erection/ejaculation prevented

Used to treat hypertension

42
Q

What is Trihexyphenidyl?

A

Muscarinic Antagonist

Specificity for M1

Used for movement disorders (Parkinson’s)

CAN cross the BBB
Centrally acting

Treat tremor and rigidity in Parkinson’s
- Blocks excess cholinergic activity (excessive M1 activation is associated with cogwheel rigidity)

43
Q

What is the general functions of the M1 receptor when activated at its various locations?

A
  • Allows signal transduction from one nerve to the next

- Promotes GI tract motility via the enteric NS

44
Q

What is the general functions of the M2 receptor when activated at its various locations?

A
  • Decreases contractility of the Atria

- Decreases heart rate via the SA node (decrease conduction rate through the AV node)

45
Q

What is the general functions of the M3 receptor when activated at its various locations?

A
  • Secretion of sweat glands
  • Secretion of pulmonary glands
  • Secretion of GI glands
  • Secretion of Lacrimal glands
  • Contraction of Ciliary and Pupillary muscles (accommodation and pupil constriction)
  • Causes NO release in vascular smooth muscle (increases cGMP, leading to vasodilation)
46
Q

What protein is associated with the alpha-1 adrenergic receptors?

A

Gq GPCR

47
Q

What protein is associated with the alpha-2 adrenergic receptor?

A

Gi GPCR

48
Q

What protein is associated with the Beta-1 adrenergic receptor?

A

Gs GPCR

49
Q

What protein is associated with the Beta-2 adrenergic receptor

A

Gs GPCR

50
Q

What protein is associated with the Beta-3 adrenergic receptor

A

Gs GPCR

51
Q

What locations can you find the alpha-1 receptor?

A
  • Most Vascular Smooth muscle
  • Pupillary dilator smooth muscle
  • Prostate/urinary sphincter smooth muscle
  • Heart
52
Q

What locations can you find the alpha-2 receptor?

A
  • Some vascular smooth muscle
  • Pancreatic islet cells
  • Post-synaptic CNS neurons
  • Platelets
  • Ciliary body of the eye
  • Adrenergic and cholinergic nerve terminals
  • Fat cells
53
Q

What locations can you find the beta-1 receptor?

A
  • Heart (including SA and AV nodes)

- juxtaglomerular cells

54
Q

What locations can you find the beta-2 receptor?

A
  • Respiratory smooth muscle
  • Vascular smooth muscle
  • Uterine smooth muscle
  • Skeletal muscle
  • Liver
  • Fat cells
  • Pancreatic Islet cells
  • Ciliary body of the eye
55
Q

What is the general functions of the alpha-1 receptor when activated at its various locations?

A
  • Contraction of vascular smooth muscle –> Increased peripheral arterial and venous resistance (MAP)
  • Contraction of dilator muscle –> Pupil dilation
  • Contraction of prostatic smooth muscle and urinary sphincter smooth muscle (thus urinary retention)
  • Increases force of contraction of the heart
56
Q

What is the general functions of the alpha-2 receptor when activated at its various locations?

A
  • Platelet aggregation
  • Decreases insulin release from pancreatic islet cells
  • Inhibits neurotransmitter release at adrenergic and cholinergic nerve terminals
  • Contraction of vascular smooth muscle
  • Inhibit aqueous humor production from the ciliary body in the eye (decreasing eye pressure –> treats glaucoma)
  • Inhibits lipolysis in fat cells
57
Q

What is the general functions of the beta-1 receptor when activated at its various locations?

A
  • Increases force and rate of contraction of the heart

- Increases renin release

58
Q

What is the general functions of the beta-2 receptor when activated at its various locations?

A
  • Respiratory smooth muscle relaxation (dilates bronchioles)
  • Uterine muscles relaxation
  • Vascular smooth muscle relaxation
  • Promotes K+ uptake into the skeletal muscle (as well as systemic HYPOkalemia)
  • Activates gluconeogenesis and glycogenolysis in the liver
  • Activates lipolysis and free fatty acid release from Fat cells
  • Causes the release of Insulin from Pancreatic Islet cells
  • Activates aqueous humor production in the ciliary body (causing increased eye pressure)
59
Q

What is the general functions of the beta-3 receptor when activated at its various locations?

A
  • Relaxes the detrusor muscle of the bladder (urinary retention)
  • Activates lipolysis
60
Q

What is Phenylephrine?

A

Direct acting Adrenomimetic Drug

Alpha agonist
- Primarily acts on alpha-1 receptors

Vasoconstrictor (both arteries and veins)
- Causes increase in MAP, Systolic BP, and Diastolic BP (increased venous return)

Causes Mydriasis (pupil dilation)

Induces reflexive bradycardia
- Increased MAP activates baroreceptors which cause the heart to become reflexively bradycardic

Used clinically to dilate pupils for retinal examination

Used clinically to treat Hypotensive emergencies:

  • hemorrhagic shock
  • Overdose of antihypertensives
  • CNS depressants

Used clinically to treat nasal decongenstion
- Vasoconstriction of nasal vessels reduces edema in nasal mucosa

61
Q

What is norepinpehprine?

A

Direct acting Adrenomimetic Drug

Specificity for alpha receptors over beta receptors (but does interact with both)

Increases cardiac contractility
- Beta-1 activity

Potent Vasoconstrictor
- Increases TPR and BP (MAP, Systolic, and diastolic BP)

Lacks Beta-2 agonist effects (no bronchodilation, no vasodilation)

Induces reflexive bradycardia
- Increased MAP activates baroreceptors which cause the heart to become reflexively bradycardic

Clinically used to treat Hypotensive emergencies:

  • Hemorrhagic shock
  • Overdose of antihypertensives
  • CNS Depressants

Colin CPR II (12 decks)

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