Nervous System - Common receptors, substrates, inhibiors, enzymes

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MOA of drugs and receptors

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– Tip Gal p. 46 - dopamine

MOA of each meds
Plus Indication

– Tip Gal p. 46
MOA: block dopamine receptor in the CNS, including the chemoreceptor trigger zone.

Metoclopramide (Reglan) &
1st gen antipsychotic: Haloperidol (MOA: mainly blocks D2 w/ 5-HT2A.

- Indication: CINV

<p>– Tip Gal p. 46 <br>MOA: <u>block dopamine receptor</u> in the <span style="color: rgb(0, 0, 0);"><mark data-color="#f8f08a" style="background-color: rgb(248, 240, 138); color: inherit;">CNS</mark></span>, including the <span style="color: rgb(239, 130, 52);"><u>chemoreceptor trigger zone</u></span>.<br></p><ul><li><p><span style="color: rgb(0, 0, 0);"><strong><mark data-color="#64a8f1" style="background-color: rgb(100, 168, 241); color: inherit;">Metoclopramide (Reglan)</mark></strong></span><strong> </strong>& </p></li><li><p>1st gen antipsychotic:<strong> </strong><span style="color: rgb(123, 236, 93);"><strong>Haloperidol</strong></span><strong> </strong>(MOA: mainly blocks <u>D2</u> w/ 5-HT2A.</p></li></ul><p>- Indication: CINV</p>

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Tip Gal p. 46

Class: (2)
MOA (2)

Tip Gal p. 46

Pilocarpine: Class: Cholinergic (Miotics): increase aqueous humor outflow
bethanechol: Class: Cholinergic (Miotics): acts on M3 receptors:

MOA: improves bladder smooth muscles: To promote emptying of the urinary bladder

<p>Tip Gal p. 46<br></p><img src="http://127.0.0.1:60866/bandicam%202025-03-31%2020-27-30-688.jpg" data-width="25%" data-align="center"><p><br><span style="color: rgb(75, 217, 114);"><strong>Pilocarpine</strong></span>: Class: Cholinergic (Miotics): <u>increase</u> <span style="color: rgb(0, 0, 0);"><mark data-color="#aef3f1" style="background-color: rgb(174, 243, 241); color: inherit;">aqueous humor</mark></span> <span style="color: rgb(189, 73, 73);">outflow</span><br><span style="color: rgb(191, 239, 105);">bethanechol</span>: Class: Cholinergic (Miotics): acts on M3 receptors: </p><ul><li><p>MOA: improves bladder smooth muscles: To promote <u>emptying</u> of the<strong> urinary bladder</strong></p></li></ul><p></p>

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<p><span>Tip Gal p. 46 - nicotinic</span><br><span>- main location?</span></p>

Tip Gal p. 46 - nicotinic
- main location?

Tip Gal p. 46
- Location: Nm = on skeletal muscles

<p>Tip Gal p. 46 <br>- Location: Nm = on <span style="color: rgb(135, 4, 16);">skeletal muscles</span></p>

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<p><span>Tip Gal p. 46 - alpha 1</span><br><span>- main location?</span></p>

Tip Gal p. 46 - alpha 1
- main location?

- location: Smooth muscles, including blood vessels
MOA: ↑ Vasoconstriction = ↑ BP
Phenylephrine: alpha-1 agonist
dopamine: alpha-1 agonist; High dose: 10-20 mcg/kg/min

<p>- location: <span style="color: rgb(195, 59, 59);">Smooth muscles</span>, including <span style="color: rgb(235, 12, 12);">blood vessels</span><br>MOA: ↑ <strong>Vasoconstriction</strong> = <strong>↑</strong> <strong>BP</strong><br>Phenylephrine: <span style="color: rgb(45, 235, 86);">alpha-1</span> agonist<br><u>dopamine:</u> <span style="color: rgb(45, 235, 86);">alpha-1</span> agonist; High dose: 10-20 mcg/kg/min</p>

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<p><span>Tip Gal p. 46 - alpha 2</span><br><span>- main location?</span></p>

Tip Gal p. 46 - alpha 2
- main location?

Tip Gal p. 46
- location: Brains & CNS --> sends signal to --> PNS [Voluntary: somatic (muscle), Involuntary: Autonomic (GI & Cardiovascular)]
↓BP (means ↑vasodilation)
Brimonidine: MOA: increase aqueous humor outflow, reduce aqueous humor production.

<p><span>Tip Gal p. 46</span><br><span>- location: </span><span style="color: rgb(51, 97, 218);">Brains</span><span> & </span><span style="color: rgb(158, 31, 138);">CNS</span><span> --> sends signal to --> PNS [Voluntary: </span><span style="color: rgb(117, 9, 53);">somatic (muscle)</span><span>, Involuntary: Autonomic (</span><span style="color: rgb(42, 156, 98);">GI</span><span> & </span><span style="color: rgb(245, 8, 8);">Cardiovascular</span><span style="color: rgb(246, 244, 244);">)</span><span>]</span><br><span> ↓BP (means ↑vasodilation)</span><br><span style="color: rgb(164, 32, 129);">Brimonidine</span><span>: MOA: </span><span style="color: rgb(106, 41, 41);">increase</span><span> </span><mark data-color="#6ec6f5" style="background-color: rgb(110, 198, 245); color: inherit;">aqueous humor</mark><span> </span><span style="color: rgb(106, 41, 41);">outflow</span><span>, </span><span style="color: rgb(57, 64, 183);">reduce</span><span> <mark data-color="#6ec6f5" style="background-color: rgb(110, 198, 245); color: inherit;">aqueous humor</mark> </span><span style="color: rgb(39, 54, 119);">production</span><span>. </span></p>

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<p><span>Tip Gal p. 46 - beta 1</span><br><span>- main location?</span></p>

Tip Gal p. 46 - beta 1
- main location?

Tip Gal p. 46
- location: Heart muscle
Dobutamine: class: Inotropes; increase the contractility. MOA: beta-1 agonist
Isoproterenol: is a mixed beta-1 and beta-2 agonist; indication: bradycardia and causes bronchodilation.
dopamine: beta-1 agonist; Medium dose: 5-10 mcg/kg/min

<p><span>Tip Gal p. 46 </span><br><span>- location: </span><span style="color: red;">Heart muscle</span><br><span style="color: rgb(202, 21, 95);"><strong>Dobutamine</strong></span><span>: class: Inotropes; </span><u>increase the contractility</u><span>. MOA:</span><span style="color: red;"> beta-1</span><span> agonist<u><br>Isoproterenol</u>: is a mixed </span><span style="color: red;">beta-1</span><span> and </span><span style="color: rgb(240, 159, 198);">beta-2</span><span> agonist; indication: <mark data-color="#eaa6a2" style="background-color: rgb(234, 166, 162); color: inherit;">bradycardia</mark> and causes bronchodilation. <br></span><span style="color: rgb(109, 240, 190);"><u>dopamine</u></span><u>:</u><span> </span><span style="color: red;">beta-1</span><span> agonist; Medium dose: 5-10 mcg/kg/min</span></p>

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<p><span>Tip Gal p. 46 - beta 2</span><br><span>- main location?</span></p>

Tip Gal p. 46 - beta 2
- main location?

Tip Gal p. 46
- Location: Lung; smooth muscle relaxation (bronchioles opens up alveoli to allow gas exchange between O₂ & CO₂
Isoproterenol: is a mixed beta-1 and beta-2 agonist; indication: bradycardia and causes bronchodilation.
Terbutaline is a beta-2 agonist used in acute, severe asthma exacerbations.

<p>Tip Gal p. 46<span style="color: rgb(54, 249, 89);"><br></span><span style="color: rgb(241, 248, 242);">- Location: </span><span style="color: rgb(16, 232, 148);">Lung</span>; smooth muscle relaxation (bronchioles opens up <strong>alveoli</strong> to allow <u>gas exchange</u> between <span style="color: rgb(128, 236, 180);">O<sub>2</sub> </span>& <span style="color: rgb(155, 97, 20);">CO<sub>2</sub></span><br><span style="color: rgb(166, 40, 40);">Isoproterenol</span>: is a mixed <span style="color: red;">beta-1</span> and <span style="color: rgb(240, 159, 198);">beta-2 </span>agonist; indication: bradycardia and causes <span style="color: rgb(0, 0, 0);"><mark data-color="#ee7d7d" style="background-color: rgb(238, 125, 125); color: inherit;">bronchodilation</mark></span>.<br><span style="color: rgb(93, 163, 224);">Terbutaline</span> is a <span style="color: rgb(240, 159, 198);">beta-2</span> agonist used in acute, severe <span style="color: rgb(3, 3, 3);"><mark data-color="#bceef4" style="background-color: rgb(188, 238, 244); color: inherit;">asthma exacerbations</mark></span>.</p>

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Triptan's MOA: 5-HT1 agonist; they vasoconstrict cranial blood vessels, ↓ migraine pain

<img src="http://127.0.0.1:60866/bandicam%202025-04-01%2000-26-26-334.jpg" data-width="50%" data-align="center"><p><strong>Triptan's </strong><span>MOA: </span><span style="color: rgb(231, 178, 96);">5-HT1</span><span> agonist; they </span><u>vasoconstrict cranial blood vessels</u><span>, ↓ migraine pain</span></p>

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– Tip Gal p. 46 & pdf p. 683
Low (renal) dose: Dopamine-1 agonist = renal (kidneys): 1-4 mcg/kg/min
Medium dose: beta-1 agonist = Heart muscle: 5-10 mcg/kg/min:
High dose: Alpha-1 agonist = Blood vessel: 10-20 mcg/kg/min
MOA: Penetrates the blood brain barrier (BBB) to lower Parkinson's disease symptoms.
Levodopa: [prodrug (precursor) of Dopamine]
pramipexole: Dopamine agonist

<p><span>– Tip Gal p. 46 & pdf p. 683</span><br><span>Low (</span><span style="color: rgb(147, 69, 26);">renal</span><span>) dose: </span><span style="color: rgb(147, 69, 26);">Dopamine-1</span><span> agonist =</span><span style="color: rgb(147, 69, 26);"> renal (kidneys)</span><span>: 1-4 mcg/kg/min<br>Medium dose: </span><span style="color: red;">beta-1 </span><span>agonist =  </span><span style="color: red;">Heart muscle</span><span>: 5-10 mcg/kg/min: <br>High dose: </span><span style="color: rgb(225, 88, 88);">Alpha-1</span><span> agonist = </span><span style="color: rgb(225, 88, 88);">Blood vessel</span><span>: 10-20 mcg/kg/min</span><br><span>MOA: Penetrates the </span><span style="color: rgb(91, 29, 89);"><strong>b</strong>lood <strong>b</strong>rain <strong>b</strong>arrier </span><span>(</span><span style="color: rgb(91, 29, 89);"><strong>BBB</strong></span><span>) to lower </span><span style="color: rgb(116, 25, 42);"><mark data-color="#87b5ec" style="background-color: rgb(135, 181, 236); color: inherit;">Parkinson's disease</mark></span><span> symptoms. <br></span><span style="color: rgb(12, 12, 12);"><mark data-color="#a2d1f5" style="background-color: rgb(162, 209, 245); color: inherit;"><u>Levodopa</u></mark></span><span>: [prodrug (precursor) of Dopamine]</span><br><span style="color: rgb(0, 0, 0);"><mark data-color="#e6e3ae" style="background-color: rgb(230, 227, 174); color: inherit;"><u>pramipexole</u></mark></span><span>: Dopamine agonist</span></p>

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– Tip Gal p. 46

MOA: (2)

– Tip Gal p. 46
antimuscarinic/anticholinergic: urinary incontinence & memory impairment
Oxybutynin: block acetylcholine, causes urinary incontinence b/c limits (lowers) contractions of the detrusor muscle.
Atropine: PPX/Tx: acute diarrhea b/c anticholinergic effects

<p>– Tip Gal p. 46<br><span style="color: rgb(0, 0, 0);"><mark data-color="#a0e1f2" style="background-color: rgb(160, 225, 242); color: inherit;">antimuscarinic</mark>/<mark data-color="#a7d581" style="background-color: rgb(167, 213, 129); color: inherit;">anticholinergic</mark></span>: <span style="color: rgb(123, 233, 195);">urinary incontinence</span> & <span style="color: rgb(126, 39, 90);">memory impairment</span><br><span style="color: rgb(0, 0, 0);"><mark data-color="#cdca8d" style="background-color: rgb(205, 202, 141); color: inherit;">Oxybutynin</mark></span>: <u>block acetylcholine,</u> causes <span style="color: rgb(123, 233, 195);">urinary incontinence</span> b/c <u>limits (lowers) contractions</u> of the <span style="color: rgb(163, 85, 23);">detrusor muscle</span>.<br>Atropine: PPX/Tx: acute diarrhea b/c <span style="color: rgb(0, 0, 0);"><mark data-color="#a7d581" style="background-color: rgb(167, 213, 129); color: inherit;">anticholinergic effects</mark></span></p>

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– Tip Gal p. 46
- Location: Nm = on skeletal muscles

<p>– Tip Gal p. 46<br>- Location: Nm = on <span style="color: rgb(211, 40, 33);">skeletal muscles</span></p>

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– Tip Gal p. 46
- location: Smooth muscles, including blood vessels
- ↑ vasodilation to ↓ BP
Carvedilol: beta-1 and beta-2 blocker & alpha-1 blocker
Doxazosin: non-selective alpha-1, alpha 2 blocker
phentolamine: selective alpha-1 blocker

<p>– Tip Gal p. 46<br>- location: <span style="color: rgb(236, 119, 119);">Smooth muscles</span>, including <span style="color: rgb(242, 10, 10);">blood vessels</span><br>- <strong>↑ vasodilation </strong>to<strong> ↓ BP</strong><br><span style="color: rgb(237, 105, 12);"><strong>Carvedilol</strong></span>: <span style="color: red;">beta-1</span> and <span style="color: rgb(240, 159, 198);">beta-2</span> <strong>blocker</strong> & <span style="color: rgb(45, 235, 86);">alpha-1</span> <strong>blocker<br></strong><span style="color: rgb(234, 52, 125);"><strong>Doxazosin</strong></span>: non-selective <span style="color: rgb(45, 235, 86);">alpha-1</span>, <span style="color: rgb(64, 100, 236);">alpha 2</span> <strong>blocker</strong> <br><span style="color: rgb(97, 205, 170);">phentolamine</span>: selective <span style="color: rgb(45, 235, 86);">alpha-1</span> <strong>blocker</strong> </p>

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<ul><li><p>Location: (2)</p></li><li><p>MOA (2)</p></li></ul><p></p>

Location: (2)
MOA (2)

– Tip Gal p. 46
- location: Brains & CNS --> sends signal to --> PNS [Voluntary: somatic (muscle), Involuntary: Autonomic (GI & Cardiovascular)]
Yohimbine: is used to ↑ libido & for erectile dysfunction.
- ↑ BP, HR. ADR; risk of seizures

ergot alkaloid: Constrict blood vessels in brain. tx: acute migraine headache
- non-selective agonist of 5-HT --> vasoconstriction
- block alpha 2 in brain --> ↑ SVR --> vasoconstriction

<p>– Tip Gal p. 46<br>- location: <span style="color: rgb(51, 97, 218);">Brains</span> & <span style="color: rgb(158, 31, 138);">CNS</span> --> sends signal to --> PNS [Voluntary: <span style="color: rgb(117, 9, 53);">somatic (muscle)</span>, Involuntary: Autonomic (<span style="color: rgb(42, 156, 98);">GI</span> & <span style="color: rgb(245, 8, 8);">Cardiovascular</span>)]<br><u>Yohimbine:</u> is used to ↑ <u>libido</u> & for <u>erectile dysfunction</u>.<br>- ↑ BP, HR. ADR; risk of <span style="color: rgb(136, 65, 203);">seizures</span></p><p><br><u>ergot alkaloid:</u> Constrict <span style="color: rgb(245, 8, 8);">blood vessels </span>in <span style="color: rgb(51, 97, 218);">brain</span>. tx: <span style="color: rgb(168, 117, 31);">acute migraine headache</span><br>- non-selective agonist of <span style="color: rgb(210, 62, 62);">5-HT</span> --> vasoconstriction<br>- block <span style="color: rgb(64, 100, 236);">alpha 2</span> in brain --> ↑ SVR --> vasoconstriction</p>

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– Tip Gal p. 46
- location: Heart muscle
Metoprolol: beta-1 blocker
- Indication: Migraine (PPX),
Propranolol: beta-1 and beta-2 blocker
- Indication: Migraine (PPX), Thyroid storm, tremor, anxiety
Carvedilol: beta-1 and beta-2 blocker & alpha-1 blocker

<p>– Tip Gal p. 46<br>- location: <span style="color: rgb(245, 13, 13);">Heart muscle</span><br><strong>Metoprolol</strong>: <span style="color: rgb(239, 10, 10);">beta-1</span> <strong>blocker<br></strong>- Indication: Migraine (PPX),<strong><br>Propranolol</strong>: <span style="color: red;">beta-1</span> and <span style="color: rgb(240, 159, 198);">beta-2</span> <strong>blocker</strong><br>- Indication: Migraine (PPX), Thyroid storm, tremor, anxiety<br><strong>Carvedilol</strong>: <span style="color: red;">beta-1</span> and <span style="color: rgb(240, 159, 198);">beta-2</span> <strong>blocker</strong> & <span style="color: rgb(45, 235, 86);">alpha-1</span> <strong>blocker</strong></p>

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– Tip Gal p. 46
- Location: Lung; smooth muscle relaxation (bronchioles opens up alveoli to allow gas exchange between O₂ & CO₂Compare: Indication: HTN, Portal Hypertension (of variceal bleeding)
Propranolol: beta-1 and beta-2 blocker
- Indication: Migraine (PPX), Thyroid storm, tremor, anxiety
Carvedilol: beta-1 and beta-2 blocker & alpha-1 blocker

<p>– Tip Gal p. 46<br>- Location: Lung; smooth muscle relaxation (bronchioles opens up alveoli to allow gas exchange between <span style="color: rgb(128, 236, 180);">O<sub>2</sub> </span>& <span style="color: rgb(155, 97, 20);">CO<sub>2</sub></span><sub><br></sub><strong>Compare: </strong>Indication: HTN, Portal Hypertension (of variceal bleeding)<strong><br>Propranolol</strong>: <span style="color: red;">beta-1</span> and <span style="color: rgb(240, 159, 198);">beta-2</span> <strong>blocker</strong><br>- Indication: Migraine (PPX), Thyroid storm, tremor, anxiety<br><strong>Carvedilol</strong>: <span style="color: red;">beta-1</span> and <span style="color: rgb(240, 159, 198);">beta-2</span> <strong>blocker</strong> & <span style="color: rgb(45, 235, 86);">alpha-1</span> <strong>blocker</strong></p>

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Ondansetron (5-HT3 RA): block serotonin, both peripherally on vagal nerve terminal nerve terminal and centrally in the chemoreceptor trigger zone.

- indication: GI for CINV

Quetiapine: block dopamine (D2) and serotonin (5-HT2A) receptors

- indication: Psychosis

<img src="http://127.0.0.1:60866/bandicam%202025-04-01%2000-26-26-334.jpg" data-width="25%" data-align="center"><p><br></p><p><span style="color: rgb(0, 0, 0);"><strong><mark data-color="#5ce9da" style="background-color: rgb(92, 233, 218); color: inherit;">Ondansetron</mark></strong></span><strong> (5-HT3 RA)</strong>: <u>block</u> <strong>serotonin</strong>, both <span style="color: rgb(232, 135, 135);"><u>peripherally</u></span> on <span style="color: rgb(232, 135, 135);"><u>vagal nerve terminal</u></span> nerve terminal and <span style="color: rgb(232, 116, 58);"><u>centrally</u></span> in the <span style="color: rgb(232, 116, 58);"><u>chemoreceptor trigger zone.</u></span> </p><p>- indication: GI for CINV</p><p><span style="color: rgb(0, 0, 0);"><strong><mark data-color="#71f366" style="background-color: rgb(113, 243, 102); color: inherit;">Quetiapine</mark></strong></span>: block dopamine (<u>D2</u>) and <span style="color: rgb(0, 0, 0);"><mark data-color="#f7f76c" style="background-color: rgb(247, 247, 108); color: inherit;">serotonin (<u>5-HT2A</u>)</mark></span> receptors</p><p>- indication: Psychosis</p>

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