LESSON 8: Drugs used in the Autonomic Nervous System Flashcards by Kim Grace

Q

-Has only one neuron
-No ganglion
-Voluntary, controllable
-thicker myelin sheath/heavily myelinated axon

A

Somatic Nervous System

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Q

Neurotransmitter of Somatic Nervous System

A

Acetylcholine

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Q

-Has two neurons
-Presence of ganglion (exclusive in ANS)
- Involuntary, uncontrollable
-Has a thin myelin sheath

A

Autonomic Nervous System

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Q

Autonomic Nervous System Neurotransmitter

A

Norepinephrine for Sympathetic
(Noradrenaline) and Acetylcholine for
Parasympathetic

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Q

Efferent organs (EO): Somatic Nervous System

A

Skeletal muscles

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Q

Efferent organs (EO): Autonomic Nervous System

A

Smooth muscles (such as the urinary bladder, GI
tract), cardiac muscles and exocrine glands

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Q

“Fight or Flight”

A

Sympathetic

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Q

Origin of neurons of Sympathetic

A

Thoracolumbar region

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Q

Dilation of pupils (Mydriasis)

A

Sympathetic “Fight or Flight”

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Q

Widening of mouth + Decreased salivatio

A

Sympathetic “Fight or Flight”

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Q

Decreased GIT activity (loss of peristalsis,
decreased bowel movement, constipation)

A

Sympathetic “Fight or Flight”

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Q

Increased heartbeat/contraction - tachycardia

A

Sympathetic “Fight or Flight”

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Q

Bronchodilation (dilate lungs to easily distribute
oxygen in body, compensation for adrenaline
rush)

A

Sympathetic “Fight or Flight”

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Q

Increased muscle tone (to regain strength)

A

Sympathetic “Fight or Flight”

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Q

Bladder relaxation → urinary retention

A

Sympathetic “Fight or Flight”

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Q

Piloerection (regulate body temperature,
especially if scared need iconserve heat)

A

Sympathetic “Fight or Flight”

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Q

Penis ejaculation

A

Sympathetic “Fight or Flight”

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Q

“Rest and Digest”

A

Parasympathetic

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Q

“Rest and Digest

A

Parasympathetic

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Q

Origin of neurons: Parasympathetic

A

Craniosacral region

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Q

Constriction of Pupils (Miosis)

A

Parasympathetic “Rest and Digest

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Q

Increased salivation

A

Parasympathetic “Rest and Digest

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Q

Increased GIT activity (increased
peristalsis/secretion/metabolis, increased bowel
movement, diarrhea)

A

Parasympathetic “Rest and Digest

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Q

Decreased heartbeat - bradycardia

A

Parasympathetic “Rest and Digest

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Bronchoconstriction

Parasympathetic “Rest and Digest

Bladder contraction → urination

Parasympathetic “Rest and Digest

Penis erection

Parasympathetic “Rest and Digest

Also called as “Intrinsic Nervous System”

ENTERIC NERVOUS SYSTEM

Consists of the submucosal, myenteric, and subserosal plexuses

ENTERIC NERVOUS SYSTEM

Consists of a mesh-like system of neurons that governs the function of GI tract

ENTERIC NERVOUS SYSTEM

Regulates the movement of water as well as electrolytes between the gapped lumen (?) and tissue compartments

ENTERIC NERVOUS SYSTEM

- inhibit choline transporters (anticholinergic)

Hemicholinium

- inhibit vesicle-associated transporter or VAT (anti-parasympathetic effect)

Vesamicol

inhibit docking proteins (VAMPs and SNAPs)

Botulinum toxin

found in the synaptic cleft, inhibits the acetylcholinesterase (increases effect of acetylcholine to bind in post-synapse)

Anti-acetylcholinesterase

inhibit tyrosine hydroxylase (anti-sympathetic effect)

Metyrosine

inhibits vesicular monoamine transporter (VMAT)

Reserpine

- inhibit docking proteins (VAMPs and SNAPs, exocytosis inhibitors)

Bretylium, guanethidine, guanidyl -

- inhibit norepinephrine transporter (NET), acts as a reuptake inhibitor (reabsorption or recycling)

Cocaine, tricyclic antidepressants (TCA)

SYMPATHOMIMETICS Pressor Agents

● Noradrenaline (Norepinephrine) ● Ephedrine ● Dopamine ● Phenylephrine ● Methoxamine ● Mephentermine

SYMPATHOMIMETICS Bronchodilators

● Isoprenaline ● Salbutamol (Albuterol) ● Terbutaline ● Salmeterol ● Formoterol ● Bambuterol

SYMPATHOMIMETICS CNS Stimulants

● Amphetamine ● Dexamphetamine ● Methamphetamine ● Methylphenidate

SYMPATHOMIMETICS Uterine Relaxants

● Ritodrine ● Isoxsuprine ● Salbutamol ● Terbutaline

SYMPATHOMIMETICS Cardiac Stimulants

● Adrenaline ● Isoprenaline ● Dobutamine

SYMPATHOMIMETICS Nasal Decongestants

● Xylometazoline ● Oxymetazoline ● Naphazoline ● Phenylephrine ● Phenylpropanolamine ● Pseudoephedrine

SYMPATHOMIMETICS Anorectics

● Amphetamine ● Fenfluramine ● Dexfenfluramine ● Sibutramine

α-ADRENERGIC BLOCKING DRUGS ( NON-EQUILIBRIUM TYPE

β-haloalkylamine (Phenoxybenzamine)

α-ADRENERGIC BLOCKING DRUGS : EQUILIBRIUM TYPE (Competitive Antagonists) : α1 Selective

● Prazosin ● Terazosin ● Doxazosin ● Alfuzosin ● Tamsulosin

α-ADRENERGIC BLOCKING DRUGS : EQUILIBRIUM TYPE (Competitive Antagonists) : α2 Selective

Yohimbine

Non-Selective EQUILIBRIUM TYPE (Competitive Antagonists)

Ergot alkaloids, Hydrogenated ergot alkaloids, Imidazoline, Miscellaneous

NON-EQUILIBRIUM TYPE (β1 + β2 (β-ADRENERGIC BLOCKING DRUGS)

Without ISA : ● Propranolol ● Sotalol ● Timolol With ISA: ● Pindolol With α blocking property: ● Labetalol ● Carvedilol

B. CARDIOSELECTIVE (β1) ( β-ADRENERGIC BLOCKING DRUGS)

● Metoprolol ● Atenolol ● Acebutolol ● Bisoprolol ● Esmolol ● Betaxolol ● Celiprolol ● Nebivolo

First Generation β-ADRENERGIC BLOCKING DRUG

● Propranolol ● Timolol ● Sotalol ● Pindolol

Second Generation β-ADRENERGIC BLOCKING DRUG

● Metoprolol ● Atenolol ● Acebutolol ● Bisoprolol ● Esmolol Third Generation With α

Third Generation β-ADRENERGIC BLOCKING DRUG

● Labetalol ● Carvedilol ● Celiprolol ● Nebivolol ● Betaxolol

CHOLINERGIC DRUGS (CHOLINERGIC AGONISTS)

Choline esters: ● Acetylcholine ● Methacholine ● Carbachol ● Bethanechol Alkaloids: ● Muscarine ● Pilocarpine ● Arecoline

CHOLINERGIC DRUGS (ANTICHOLINESTERASES; REVERSIBLE)

Carbamates: ● Physostigmine (Eserine) ● Neostigmine ● Pyridostigmine ● Edrophonium ● Rivastigmine ● Donepezil ● Galantamine Acridine: Tacrine

CHOLINERGIC DRUGS (ANTICHOLINESTERASES; IRREVERSIBLE)

Carbamates: ● Carbaryl (Sevin) ● Propoxur (Baygon) Organophosphates: ● Dyflos (DFP) ● Echothiophate ● Malathion (insecticide) ● Diazinon* (TIK-20) ● Tabun (nerve gases for chemical warfare) ● Sarin (nerve gases for chemical warfare) ● Soman (nerve gases for chemical warfare)

IS ATROPINE ANTIMUSCARINIC OR MUSCARINIC?

ANTIMUSCARINIC AGENTS (ANTAGONISTS)

ATROPINE Causes _____________________ blockade of cholinomimetic (mimics action of cholinergic or parasympathetic) actions at muscarinic receptors

reversible (surmountable)

When atropine binds to the muscarinic receptor, it prevents actions such as the release of_____________ and the inhibition of adenylyl cyclase that are caused by muscarinic agonists

inositol trisphosphate (IP3)

Therapeutic uses of atropin

Mydriatic, cycloplegic, Antispasmodic, Antidote for cholinergic agonist, Antisecretory agent

dilation of the pupil of the eye caused by contraction of the dilator muscle of the iris, decrease in light, action of drug

Mydriasis

paralysis of the ciliary muscles of the eye that results in the loss of visual accommodation

Cycloplegia

Scientific name of Atropine

Atropa belladonna

Natural sources of atropine

● Atropine (isomer Hyoscyamine) ● Found in Solanaceae family ○ Datura stramonium (Jamestown weed, sacred datura, thorn apple) ○ Hyoscyamus niger (henbane) ○ Mandragora officinarum (mandrake)

Muscarinic organs

nerve, heart and smooth muscles, glands and endothelium

Nicotinic organs

- neuromuscular endplate, skeletal muscles, autonomic ganglion cells

Cholinoreceptor stimulants: Direct acting

■ Alkaloids - nicotine, pilocarpine, obeline ■ Choline esters - methacholine, carbachol, bethanechol

Cholinoreceptor stimulants: Indirect acting

■ Reversible - carbamates (neostigmine, physostigmine), edrophonium ■ Irreversible - organophosphates (malathion, parathion)

reverses action of non-depolarizing neuromuscular blockers

Neostigmine

anti-alzheimer’s

Physostigmine & Edrophonium:

PILOCARPINE IS MUSCARINIC OR ANTIMUSCARINIC?

MUSCARINIC

Pilocarpine is the drug of choice for

emergency lowering of intraocular pressure of both narrow angle (closed-angle) and wide-angle (open-angle) glaucoma

Pilocarpine is contraindicated for

asthma, peptic ulcer, coronary artery diseases

Natural Sources of pilocarpine

● Rutaceae family, genus Pilocarpus, (common name Jaborandi) ● Pilocarpus pennatifolius (South American