1 Murphy N305 Pns Drugs

Front 1

Hello everyone!

So, what will we be studying?

Back 1

PNS DRUGS!!
(Peripheral Nervous System)

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ACETYLCHOLINE
Neurotransmitter

Back 2

Released from
Postganglionic receptors – Nn
Somatic – NMJ Nm
Sweat glands M (sym)
Parasympathetic target organs M

Target organs, sweat glands, and Skeletal muscle!

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NOREPINEPHINE

Back 3

Released from postganglionic neurons in most sympathetic systems

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Here are a few general questions before we get into the drugs...

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Ready?

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Simple question. What is an:

agonist?
antagonist?

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agonist: increase effects on stimulation

antagonist: blocks and decreases effects

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What does competitive and noncompetitive mean?

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competitive: can unbind by an agonist or ACh

noncompetitive: Can't be moved!! Won't budge until the body makes a new receptor

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Cholinergic Effects:
Parasympathetic

Can you tell me what "HEBUGGED" stands for?
(words in parenthesis are examples of an agonist effect)

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Heart (decrease)
Eye (meiosis - pupil shrinks)
Bronchoconstriction
Urination (increase)
GI (increase)
Glandular secretions (gooey, antiglandular is the opposite [dries up])
Erection
Dilation (vaso)

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Great job! Let's start with the drugs now.

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Don't feel overwhelmed! These note-cards will be sure to help!

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Cholinergic Drugs-->
Parasympathetic:
___ = mAChr agonist
___ = mAChr antagonist
___ = AchE inhibitor

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Parasympathetic:
BETHANECHOL = mAChr agonist
ATROPINE = mAChr antagonist
NEOSTIGMINE = AchE inhibitor (*increases effects b/c it allows ACh to linger in synapse longer!)

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BETHANECHOL [Urecholine]
Class

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Bethanechol - Class

Muscarinic receptor agonist

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Bethanechol
Mechanism of Action
*Think about it's class*

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Bethanechol - MOA

Reversibly activates muscarinic cholinergic receptors (mAChR)
Acts on: ParasympNS, sweat glands SympNS, vascular smooth muscle

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Bethanechol [Urecholine]
Therapeutic uses

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Bethanechol Tx use:

Urinary retention (ex: post-op and postpartum)
Muscarinic activation in bladder results in increase in fluid release

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Bethanechol [Urecholine]
Major Side Effects
*Activation of mAChR*

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Bethanechol SE:

-Decrease HR
-Increase sweating, salivation, and gastric acid secretions
-Bronchoconstriction and increase in GI motility
-Increase in vasodilation (may lead to hypotension)
-Increase miosis/near vision

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ATROPINE [AtroPen]
Class

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Atropine - Class

Muscarinic receptor antagonist
aka "anticholinergic" drugs

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Atropine [AtroPen]
Mechanism of Action

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Atropine MOA:

-Reversibly inhibits activation of mAChR by Ach

-Acts on therapeutic doses

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Atropine [AtroPen]
Therapeutic Uses

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Atropine - Tx:

Mydriases allows use in eye exams and eye surgery

Increase HR

Decrease in GI motility allows getting rid of abdominal cramps

Used to counter muscarinic agonist poisoning (ex: bethanachol, mushrooms)

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Atropine [AtroPen]
Major Side Effects
*Inhibits mAChR*

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Atropine SE: Can't see, can't spit, can't pee, can't sh*t!

-Increase HR (may cause tachycardia)
-Decrease in sweating (anhidrosis), salivation (xerostomia), gastric acid
-increase in urinary retention and constipation
-Blurred vision/photophobia (mydriasis/cycloplegia), increase in intraocular pressure
-CNS excitation (increase in hallucinations)

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NEOSTIGMINE [Prostigmin]
Class

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Neostigmine Class:

Cholinesterase inhibitor

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Neostigmine [Prostigmin]
Mechanism of Action

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Neostigmine MOA:

-Reversibly inhibits AChE

-tx levels, will only effect mAChR (same as mAChR agonists) & nAChR or NMJ (increase force of contraction)

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Neostigmine [Prostigmin]
Therapeutic Uses

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Neostigmine Tx:

-Myasthenia gravis (increasing ACh at NMJ, leads to increase in muscle strength)

-Reverses effects of tubocurarine (by increasing ACh at NMJ)

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Neostigmine [Prostigmin]
Major Side Effects

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Neostigmine SE:

Same SE as bethanechol

Excessive ACh accumulation in NMJ = paralysis (ex: respiratory muscles)

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Cholinergic Drugs -->
Somatic SM muscle:
___ = Nm blocker (competitive)
___ = Neuromuscular (noncompetitive)
* which Parasympathetic drug is also in this category?

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Somatic SM muscle:
Tubocurarine = Nm blocker
Succinylcholine = Neuromuscular
* Neostigmine!

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TUBOCURANINE
Class

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Tubocuranine - Class

Competitive neuromuscular blocker (ex: nondepolarizing)

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Tubocuranine
Mechanism of Action

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Tubocuranine - MOA

Competitively inhibits ACh from binding to nicotinic m receptors (prevents ACh from stimulating muscle contraction)

(+) molecule --> can't cross blood-brain barrier; no CNS effects

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Tubocuranine
Therapeutic uses

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Tubocuranine -Tx

↑muscle relaxation (ex: flaccid paralysis)

Used during surgery, mechanical ventilation, & endotracheal intubation

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Tubocuranine
Major Side Effects

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Tubocuranine - SE

Respiratory depression/arrest (reversed by AChE inhibitor)

↓BP, ↓HR

Does NOT effect CNS (ex: doesn't diminish consciousness or perception of pain)

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SUCCINYLCHOLINE [Anectine]
Class

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Succinylcholine - Class

Depolarizing neuromuscular blocker

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Succinylcholine [Anectine]
Mechanism of Action

* - important

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Succinylcholine - MOA

Ultra-short-acting drug (compared to tubocurarine)

Binds to nicotinic m receptors (and initially activates receptor --> *initial/ transient muscle contractions (i.e. *fasciculations) but does not readily release from nAChR, thus preventing ACh from binding; prevents subsequent contractions

No CNS effects - Same reason as Tubocurarine

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Succinylcholine [Anectine]
Therapeutic Uses

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Succinylcholine - Tx

↑muscle relaxation (i.e. flaccid paralysis)

Used for short procedures (ex: endotracheal intubation, endoscopy)

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Succinylcholine [Anectine]
Major Side Effects

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Succinylcholine - SE

Malignant hyperthermia
Post-op muscle pain
Does NOT effect CNS (ex: ___)

Front 31

Great going guys!
Let's go over some basic info on: Adrenergic agonists and Beta 1 and 2 tx uses

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Let-sa-go!

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Adrenergic Agonists
2 versions
What are they?

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Catecholamines - E, NE, isoproterenol, dobutamine, dopamine

Noncatecholamines - Ephedrine, Phenylephrine, Terbutaline

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Catecholamines: E, NE, isoproterenol, dobutamine, dopamine

Give me 3 facts!

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-Cant be used orally
-Can’t pass BBB b/c they are polar molecules so it doesn’t affect brain
-Very short half-life

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Noncatecholamines – Ephedrine, Phenylephrine, Terbutaline

Give me another 3 facts!

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-Can be given orally
-Less polar, can pass BBB
-Longer half-life

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Selectivity is affected by the ____ of drug

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Selectivity is affected by the amount of drug.

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Now, we'll group these Adrenergic Agonists into 2 groups. The Alpha 1 and the Alpha 2 group. Can you tell me which alpha is affected by what?

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ALPHA 1 - E, NE, Ephedrine, Phenylephrine, Dopamine

ALPHA 2 – E, NE, Ephedrine

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Alpha 1 - E, NE, Ephedrine, Phenylephrine, Dopamine

Tx and SE?

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Vasoconstriction in BV of skin, viscera, mucous membranes, and mydriases.
This stops hemostasis (E topical), causes nasal decongestion (ephedrine orally), and increases BP in hypotensive pts

SE: HTN, necrosis, and Bradycardia

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ALPHA 2 – E, NE, Ephedrine

Tx and SE?

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Activation inhibits NE release but has lil clinical sig.

CNS - reduction of sympathetic outflow of heart and BV. This is Sig.

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Now, we'll group these Adrenergic Agonists into 2 groups. The Beta 1 and the Beta 2 group. Can you tell me which beta is affected by what?

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Beta 1 - Affected by: E, NE, Ephedrine, Dopamine, Dobutamine, Isoproterenol

Beta 2 - Affected by: E, Ephedrine, Isoproterenol, terbutaline

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Beta 1 - Affected by: E, NE, Ephedrine, Dopamine, Dobutamine, Isoproterenol

Tx and SE

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Beta 1 - Heart and Kidneys (increase contractilities and renin)

Tx: How does that help the following? Cardiac arrest (Not often but if so, E is used.), heart failure, shock.

SE: tachycardia and dysrhythmias, angina pectoris
**Renal beta receptors not associated w/beneficial or adverse effects

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Beta 2 - Affected by: E, Ephedrine, Isoproterenol, terbutaline

Tx and SE

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Beta 2 - affects Lungs, Liver, and SM

Tx: Asthma (inhale terbutaline), relax uterine SM of uterus todelay preterm labor

SE: Hyperglycemia - promote glycogen breakdown and insulin maintains blood glucose (occurs in diabetic pts)
Tremors - due to SM contractions. generally fades.

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The only one you need to learn is: Epinephrine
What is is again?

Back 42

Adrenergic receptor agonist

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EPINEPHRINE
Mechanism of Action

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Epinephrine - Mechanism of Action
Sympathetic-acting drug; activates all alpha 1,2 and beta 1,2 receptors

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Epinephrine
Therapeutic Use

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Epinephrine - Tx uses
-α 1 -Vasoconstriction- Slows absorption of local anesthetic; ↓superficial bleeding; ↓nasal decongestion; ↑BP, mydriasis
-β 1-Restores cardiac function in pts in cardiac arrest
-β 2-↑bronchodilation in pts with asthma
-tx for anaphylactic shock (a combination of alpha & beta effects)

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Epinephrine
Major Side Effect r/t to MOA

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Epinephrine - SE r/t to MOA
-HTN; angina pectoris (pain due to inadequate blood flow and oxygenation to heart muscle. Usually due to atherosclerosis or high physical activity or a large meal, cold weather, stress), dysrhythmia, necrosis w/extravasation
-Hyperglycemia (high blood sugar levels) in diabetic pts (because β2 activation in liver/skeletal muscle -> breakdown of glycogen)

Front 46

Epinephrine
Routes of administration

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Epinephrine - Routes of administration

Topical, injection, inhalation, intracardiac, intraspinal

Front 47

Okay then. We've been talking about stimulating alpha and beta receptors. Now, we'll go over "Antagonists". Blocking Alpha and Beta receptors.

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After these antagonists, you'll be done!

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Adrenergic Antagonists (All are reversible)

Main use/Tx:

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Adrenergic Antagonists
Main use:
BV, bladder, prostate
Tx: **Essential HTN, Reverse toxicity of alpha agonist, benign prostatic Hyperplasia, pheochromocytoma, Raynaud's disease**
Think/discuss with others about why adrenergic antagonists are therapeutic for these.

Front 49

Adrenergic Antagonists
Side effects:

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Adrenergic Antagonists SE:
Alpha 1 - Orthstatic hypotension (reduce blood flow to brain, reflex tachycardia due to baroreceptor reflex, nasal congestion, inhibition of ejaculation but reversible, Na retention and increase BV/BP)
Alpha 2 - can intensify reflex tachycarda b/e NE increase

Front 50

Now you know ALL about Adrenergic Antagonists. The drug you need to know is: PRAZOSIN [Minipress]. What's it's class again?

Back 50

Prazosin - Class
Alpha 1 adrenergc receptor antagonist
*often causes postural hypotension

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Prazosin [Minipress]
Mechanism of Action

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Prazosin MOA

Selective competitive antagonist of alpha1 adrenergic receptor --> dilation of arterioles & veins; relaxation of smooth muscle in bladder

Front 52

Prazosin [Minipress]
Therapeutic Use

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Prazosin Tx:

HTN, Benign prostatic hyperplasia (b/c of muscle relaxation effects in bladder)

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Prazosin
Pharmacokinetics

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Prazosin Pharmacokinetics

Oral
Half life 2-3 hrs
Effects peak in 1-3 hrs and persists up to 10 hrs

Front 54

Prazosin
Major Side Effects r/t MOA

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Prazosin SE r/t MOA
You know it!
Orthostatic hypotension, reflex tachycardia, nasal congestion

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Blocking Beta Receptors

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You'll be learning about Propranolol and Metopolol. However, lets first go over their main uses, Tx, and SE

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Blocking Beta Receptors
Main Use/Tx

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Blocking Beta Receptors
Main use: reduce HR, force of contraction, velocity of impulse conduction through the AV node
Tx: Angina pectoris, hypertension, cardiac dysrhythmias, MI, Hyperthyroidism, migraine, stage fight, pheochromocytoma, glaucoma

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Blocking Beta Receptors
Side Effects

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Blocking Beta Receptors SE:
Beta 1: Bradycardia, ↓ CO, precipitation of HF (also used to treat), AV heart block (suppression of impulse conduction through the AV node), rebound cardiac excitation
Beta 2: Bronchoconstriction, inhibition of glycogenolysis (E, acting on beta2 receptors in SM and liver, will breakdown glycogen into glucose)

Front 58

PROPRANOLOL [Inderal]
Class

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Propranolol Class
beta1 and beta2 Adrenergic receptor antagonist

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Propranolol
Mechanism of Action

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Propranolol MOA (competitive antagonist)
Heart- ↓ HR, contractility, CO
Kidney - ↓ renin, BP
Lungs -↑ bronchoconstriction
BV - ↑ vasoconstriction
Liver/skeletal muscle - ↓ glycogenolysis

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Propranolol
Therapeutic Use - Oral

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Propranolol Tx:

HTN, angina pectoris, dysrhythmias, myocardial infarction (opposite of agonizing beta 2)

Stage Fright

Front 61

Propranolol
Major Side Effects

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Propranolol SE:

-↓HR; heart failure
-bronchoconstriction
-inhibition of glycogenolysis
-CNS effects (can cross blood-brain barrier because of lipid solubility)

Front 62

METOPROLOL [Lopressor]
Class

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Metoprolol Class:
beta1(selective) adrenergic receptor antagonist
AKA cardioselective beta AR antagonist

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Metoprolol
Mechanism of Action

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Metoprolol MOA:
-block beta 1 AR (found in heart [↓ HR, contractility, Av conduction velocity] and kidney[↓ renin secretion])

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Metoprolol
Therapeutic Use

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Metoprolol Tx:

HTN (MAIN use)
Angina pectoris

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Metoprolol
Major Side Effects

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Metoprolol SE:
Bradycardia, ↓CO, AV heart block, rebound cardiac excitation (following withdrawal)

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Wonderful! You've finished!
~You hear people clapping for you and patting you on the back~

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Want to just quickly go over the drugs you have learned? Sure! Why Not!?

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Parasympathetic

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Parasympathetic:
Bethanechol (mAChr agonist)
Atropine (mAChr antagonist)
Neostigmine (AChE inhibitor)

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Somatic SM

Back 68

Somatic SM:
Tubocurarine (Nm blocker)
Succinylcholine (Neuromuscular)

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Alpha & Beta Receptors Agonists: ? (1)

Alpha & Beta Receptors Antagonists: ? (3)

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Alpha/Beta agonist: Epinephrine

Alpha/Beta antagonist:
Alpha - Prazosin
Beta - Propranolol
Metoprolol

Front 70

Wow! A total of 9 drugs! Great Job Buddies!

=)

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Study Study Study....