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Neuro > ANS - just the drugs and targets > Flashcards

ANS - just the drugs and targets Flashcards

1
Q

What are the 7 important Cholinergic Agonists?

A 
Pilocarpine - M
bethanechol - M
(the rest are ache inhibitors)
neostigmine
pyridostigmine
edrophonium
donepezil
organophosphate nerve gas
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2
Q

What are the 10 important Cholinergic Antagonists?

A

7 are antimuscarinics
atropine, scopolamine, benztropine, oxybutynin, tolterodine, ipratropium, tiotropium
3 are antinicotinics (NMJ)
atracurium, rocuronium, succinylcholine

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3
Q

Propantheline is what type of drug?

A
  • Semisynthetic antimuscarinic

* Quaternary ammonium and thus relatively greater effect on GI motility

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4
Q

Glycopyrrolate is what type of drug?

A
  • Semisynthetic antimuscarinic

* Quaternary ammonium and thus relatively greater effect on GI motility

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5
Q

Benztropine is what type of drug?

A
  • Semisynthetic antimuscarinic

* Tertiary amine compounds so there is potential for CNS involvement

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6
Q

Oxybutynin is what type of drug?

A
  • Semisynthetic antimuscarinic

* Tertiary amine compounds so there is potential for CNS involvement

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7
Q

Tolterodine is what type of drug?

A
  • Semisynthetic antimuscarinic

* Tertiary amine compounds so there is potential for CNS involvement

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8
Q

Scopolamine is what kind of drug?

A

• A naturally occuring, alkaloid antimuscarinic

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9
Q

Hexamethonium is considered what type of drug?

A

• Ganglionic blocker, antinicotinic, anticholinergic

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10
Q

Atropine is considered what type of drug?

A

• Non selective antimuscarinic anticholinergic

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11
Q

Pralidoxime is considered what type of drug?

A

• Cholinesterase regenerator, anticholinergic (indirect)

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12
Q

Pirenzepine is considered what type of drug?

A

• M1 selective antimuscarinic anticholinergic

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13
Q

What does the drug Edrophonium do?

A

• Reversible, short acting ache inhibitor

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14
Q

what is special about pilocarpine?

A

It is highly lipophilic and can distribute anywhere, CNS or periphery

  • that means any muscarinic receptor in the body is a target for pilocarpine
  • also it is not ache degraded, only secreted by kidneys and trapped by acidic urine
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15
Q

What are the 8 important adrenergic agonists?

A 
Each has a different receptor profile
Epinephrine - alpha1, alpha2, beta1, beta2
Norepinephrine - alpha1, alpha2, beta1
isoproterenol - beta1, beta2
albuterol - beta2
phenylephrine - alpha1
pseudoephedrine - indirect agonist
dobutamine - beta1
dopamine - D1 (important for renal vasculature), also an indirect SNS agonist
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16
Q

What are the 9 important adrenergic antagonists?

A 
Doxazosin, Terazosin, Prazosin - alpha1
Metoprolol, Atenolol - beta1
Propanolol - beta1, beta2
Labetalol, Carvedilol - alpha1, beta1, beta2
Clonidine - alpha2 AGONIST
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17
Q

When an alpha2 adrenergic receptor is bound, what happens?

A
  • Alpha2 receptor = Gi protein.
    • cAMP is decreased as AC is inhibitied
    • K channel opening is also a possible event
    • When you see any Gi for neuro, think hyperpolarization
    • The nerve terminal will be LESS ACTIVE
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18
Q

What kind of GPCR is the beta2 adrenergic receptor?

A
  • Gs - increases AC, increasing cAMP (probably closing the K channel)
    • End result is a positive nerve terminal response
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19
Q

What kind of GPCR is the beta1 adrenergic receptor?

A
  • Gs - increases AC, increasing cAMP (probably closing the K channel)
    • End result is a positive nerve terminal response
    • Also Beta1 stimulation increases Ca conductance through L and N type Ca channels
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20
Q

What kind of GPCR is the alpha2 adrenergic receptor?

A
  • Gi - inhibits AC, reducing cAMP and often opening a K channel
    • End result is hyperpolarization of the nerve terminal
21
Q

What kind of GPCR is the alpha1 adrenergic receptor?

A

• Gq - active PLC, release IP3 and DAG, releasing intracellulr calcium and activating PKC

22
Q

For adrenergic agonists, what is the most common mechanism of indirect-acting agonists?

A

• At peripheral synapses, increasing the storage and release of NE/EPI is the most common mechanism of increasing SNS output by indirect means

23
Q

What determines absorption by oral route of SNS agonists?

A
  • Ability to resist first pass metabolism
    • MAO and COMT in the liver
    • Methyl group on alpha-carbon helps - escape MAO
    • Non-catechols helps (no OH groups on phenyl ring) - escape COMT
24
Q

Due to the molecular properties of SNS agonist drugs, what is the end result of their bioavailability?

A
  • Catecholamine NT (NE and EPI) are not effective orally
    • They also don’t enter the brain well
    • Have short durations of action
    • If you design a drug you have to strategically overcome these issues
25
Q

What property of adrenergic SYMPATHOLYTIC antagonists greatly LIMITS their clinical utility?

A

• Lack of specificity
• They work at all adrenergic synapses
*thus we use adrenergic receptor blockers more than sympatholytic drugs
*these drugs work by modulating pre-synaptic nerve terminal thus they lose specificity

26
Q

What are the two non-selective alpha adrenergic receptor blockers?

A
  • Phentolamine and phenoxybenzamine

* Irreversible alpha1 and alpha2 blockers

27
Q

What does alpha2 receptor activation do?

A

• CNS - stimulation of postsynaptic cells in the brain stem vasomotor center
○ Reduced peripheral SNS activity
• SNS - preferentially stimulates peripheral alpha2 (presynaptic) receptors
○ Reduces NE release from sympathetic neurons
• Overall, alpha2 receptors reduce SNS activity

28
Q

What does the ANS do in the eye?

A

alpha1 adrenergic receptor - contraction of iris radial muscle, dilates the pupil
muscarinic receptor - contraction of iris sphincter muscle (pupil contracts), contraction of ciliary muscle (lens accommodates for near vision)

29
Q

What does the ANS do in the trachea and bronchioles?

A

beta2 adrenergic receptor - dilates the airways

muscarinic receptors - constricts airways, increases secretions

30
Q

What does the ANS do in the adrenal medulla?

A

nicotinic neruonal receptors - epinephrine and norepinephrine is secreted - has SNS effects, all adrenergic receptors are bound

31
Q

What does the ANS do in the kidney?

A

beta1 adrenergic receptor - secretion of renin

alpha1 adrenergic receptor - decreases secretion of renin

32
Q

What does the ANS do in the ureters and bladder?

A

beta2 adrenergic receptor - relaxes detrusor, contraction of trigone and sphincter
alpha1 adrenergic receptor - relaxes detrusor, contraction of trigone and sphincter
muscarinic receptor - contraction of detrusor, relaxation of trigone and sphincter (micturate)

33
Q

What does the ANS do in the genitalia?

A

MALE
muscarinic - stimulates erection
alpha1 adrenergic receptor - stimulates ejaculation

34
Q

What does the ANS do in the lacrimal glands?

A

muscarinic only - stimulates tears

35
Q

What does the ANS do in the salivary glands?

A

alpha1 adrenergic receptor - thick viscid secretion

muscarinic receptor - copious, watery secretion

36
Q

What does the ANS do in the heart?

A

beta1 adrenergic receptor - increased rate, increased contractility
M2 muscarinic receptor - decreased rate, decreased contractility

37
Q

What does the ANS do in the GI tract?

A

beta2 adrenergic receptor - decrease in muscle motility and tone
alpha1 adrenergic receptor - contraction of sphincters
muscarinic receptors - increased muscle motility and tone

38
Q

What does the ANS do in the genitalia (female)?

A

beta2 adrenergic receptor (SNS)

*relaxation of uterus

39
Q

What does the ANS do in the Blood vessels (skelatal muscle)?

A

beta2 adrenergic receptor (SNS)

*dilation and drop in TPR

40
Q

What does the ANS do in the blood vessels (skin, mucous membranes and splanchnic area)?

A

alpha1 receptor

*constriction - leads to a rise in TPR

41
Q

What is my mneumonic for remembering the 8 important adrenergic agonists?

A 
Everybody - Epinephrine
Noses - Norepinephrine
In - Isoproterenol
All - albuterol
Possible - phenylephrine
Personal - pseudoephedrine
Dirty - dobutamine
Details - dopamine
42
Q

What is my mneumonic for remembering the 9 important adrenergic ANTagonists?

A 
Dinger - doxazosin
Tries (to) - terazosin
Poop - Prazosin
Meticulously - metoprolol
Avoiding - atenolol
Popular - propanolol
Locations, - labetalol
Certainly - carvedilol
California - clonidine
43
Q

What adrenergic receptor is predominant in uterine smooth muscle?

A

Beta2 receptor

44
Q

What adrenergic receptor is predominant in the urinary bladder sphincter?

A

alpha1 receptor - increases tone, or prevents urination

45
Q

What adrenergic receptor stimulates the release of renin?

A

Beta1 receptor - in balance with alpha1 receptor

46
Q

What adrenergic receptor is responsible for pupil dilation?

A

alpha1 receptor

47
Q

Which receptors are important for IOP?

A

IOP = intraocular pressure
alpha1 = decrease IOP through outflow of humor
Beta1, Beta2 = increase IOP through increased humor production

48
Q

according to French, which receptor blockade is best for relieving BPH-related urinary symptoms?

A

alpha1 antagonist

  • this surprised me as I thought Beta1 was more involved in the relaxing of detrusor and tightening trigone and sphincter
  • just remember BPH urinary urgency, diminished stream, block alpha1 (-azosins like Doxazonsin, Prazosin, Terazosin)

Neuro (59 decks)

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