COLLEGE OF MEDICINE & HEALTH SCEINCES

Autonomic Nervous system drugs for 2nd year Nurse

students

By Solomon Asmamaw
(B.Pharm., MSc.)

August, 2022
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Objectives

At the end of the lesson students will be able to explain:

Effects of parasympathetic and sympathetic nervous

system on tissues or organs of the body

Adrenergic agonists and antagonists

Cholinergic agonists and antagonists

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 Nervous system

Central Nervous
System
Human Nervous
system
Peripheral
Nervous System

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Includes neurons and Peripheral
ganglia outside of the Nervous
brain and spinal cord
System

ANS Controls Either *Autonomic Somatic Nervous

“fight and flight ” Nervous System System
or “rest and digest” (involuntary) (voluntary)

With Sympathetic Parasympathetic

neurotransmitters Nervous System Nervous System
norepinephrine (adrenergic) (cholinergic)
and acetylcholine

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What are Neurotransmitters?

Neurotransmitters are often referred to as the body’s

chemical messengers

 Which Transmit messages

between neurons

from neurons to muscles or glands

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Types of neurotransmitters

Over 100 signal molecules in the nervous system have

been identified

 Norepinephrine, Acetylcholine, dopamine, serotonin,

histamine, glutamate, and γ-aminobutyric acid (GABA),
endorphins are most commonly involved in the actions
of therapeutically useful drugs

 Acetylcholine and norepinephrine are the primary

chemical signals in the ANS
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What are neurons?

A neuron is a nerve cell that is the basic building blocks of

the nervous system

Designed to transmit information to other nerve cells,

muscle, or gland cells

Types of neurons

 Sensory neuron

 Motor neuron

 Interneuron

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The adrenergic neurons

 Adrenergic neurons are neurons which use epinephrine &

norepinephrine to send messages

 These neurons are found in the

CNS

sympathetic nervous system

 Adrenergic drugs act on adrenergic receptors, located either

presynaptically on the neuron or postsynaptically on the
effector organ

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Adrenergic receptors (adrenoceptors)

 Are receptors in which adrenergic neurotransmitters

epinephrine and norepinephrine binds with

 Two main families of receptors, designated α & β

Alpha (α)—α1 and α 2

Beta (β)—β1, β2, β3

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 Location &functions of adrenergic receptors

Alpha 1(α1) receptors

Located on blood vessels, kidney, liver, uterus, male sexual

organs, intestinal smooth muscle, pupillary dilator muscle

Activation of Alpha 1 receptors

 Causes vasoconstriction, decreased renin secretion,

causes uterine contraction, mydriasis

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Alpha 2 (α 2) receptors

 Found presynaptically on the neuron

 Inhibits release of norepinephrine in the form of negative

feedback

affects vascular smooth muscle, inhibits insulin

secretion, platelet aggregation, inhibits aqueous humor

formation

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Beta 1(β1) receptors
Found on heart and kidney
 affects contractility of heart and renin release by
the kidneys
Beta 2 (β2) receptors
Ciliary muscle of eye, lung, kidney, blood vessel
 Accommodation for distant vision, Enhance
aqueous humor formation, affects lungs, liver,
blood vessel vasodilation, decreased motility and
tone
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Sympathetic nervous system

The sympathetic nervous system directs the body's rapid

involuntary response to dangerous or stressful situations

 Has the property of adjusting in response to stressful

situations

such as trauma, fear, hypoglycemia, cold, & exercise

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Sympathetic responses of the body
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Adrenergic agonists (symphatomimetics)

Characteristics of adrenergic agonists

 Most of the adrenergic drugs are derivatives of β-

phenylethylamine

Substitutions on the benzene ring or on the ethylamine

side chains produce a variety of compounds with varying

abilities to differentiate between α and β-receptors and to

penetrate the CNS

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Figure. Structures of several important adrenergic agonists
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  Based on:

 The number and location of OH substitutions on the

benzene ring

The drugs can be classified

1. Catecholamines

2. Non-Cathecolamines

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Catecholamines

Epinephrine

Norepinephrine

Isoproterenol

Dopamine

 Sympathomimetic amines that contain the 3,4-

dihydroxybenzene group

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 These compounds share the following properties

High potency

 show the highest potency in directly activating α or β receptors

Rapid inactivation

 Catecholamines are metabolized by COMT postsynaptically and

by MAO intraneuronally, as well as by COMT and MAO in the
gut wall, and by MAO in the liver

 Thus, catecholamines have only a brief period of action

when given parenterally

 They are inactivated (ineffective) when administered orally

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Poor penetration into the CNS

 Catecholamines are polar and, therefore, do not readily

penetrate into the CNS

 Nevertheless, most catecholamines have some clinical effects

(anxiety, tremor, and headaches) that are attributable to action

on the CNS

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Non-catecholamines
Phenylephrine
Ephedrine
Amphetamine
Compounds lacking the catechol hydroxyl groups have
longer half-lives
 because they are not inactivated by COMT & MAO
Increased lipid solubility of many of the non
catecholamines (due to lack of polar hydroxyl groups)
permits greater access to the CNS
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Substitutions on the amine nitrogen

 The nature of the substituent on the amine nitrogen is

important in determining β selectivity of the adrenergic agonist

 epinephrine, with a –CH3 substituent on the amine nitrogen,

is more potent at β receptors than norepinephrine, which
has an unsubstituted amine

 Isoproterenol, which has an isopropyl substituent–CH

(CH3)2 on the amine nitrogen is a strong β agonist with little
α activity

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Mechanism of action of adrenergic agonists

 Direct-acting agonists (Catecholamines)

 Indirect-acting agonists (non-cathecolamines)

 Mixed-action agonists (non-cathecolamines)

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Figure. Sites of action of direct-, indirect-, and mixed-acting adrenergic agonists

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Actions

Cardiovascular

 Strengthens the contractility of the myocardium (positive inotrope:

β1 action)

 Increases its rate of contraction (positive chronotrope: β1 action)

 cardiac output increases &increase oxygen demands on the

myocardium

 activates β1 receptors on the kidney to cause renin release

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  constricts arterioles in the skin, mucous membranes, and
viscera (α1 effects)

 dilates vessels going to the liver and skeletal muscle ( β2

effects)

 Renal blood flow is decreased

 Therefore, the cumulative effect is an increase in systolic

blood pressure, coupled with a slight decrease in diastolic
pressure due to β2 receptor–mediated vasodilation in the
skeletal muscle vascular bed

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Respiratory

Causes powerful bronchodilation (β2 action)

Inhibits the release of allergy mediators such as histamines

from mast cells

Hyperglycemia

has a significant hyperglycemic effect because of

 increased glycogenolysis in the liver (β2 effect)

 increased release of glucagon ( β2 effect)

 decreased release of insulin (α2 effect)

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Lipolysis

 Initiates lipolysis through agonist activity on the β3-receptors

of adipose tissue

 Increased levels of cAMP stimulate a hormone-sensitive

lipase, which hydrolyzes triglycerides to free fatty acids and

glycerol

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Therapeutic uses

Bronchospasm

 Used in the emergency treatment of respiratory conditions

when bronchoconstriction has resulted in diminished

respiratory function

 Thus, in treatment of acute asthma and anaphylactic shock

(Epinephrine is the drug of choice)

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Anaphylactic shock

 For the treatment of type I hypersensitivity reactions (including

anaphylaxis) in response to allergens (Epinephrine)

Cardiac arrest

 Used to restore cardiac rhythm in patients with cardiac arrest

Anesthetics

 Greatly increases the duration of local anesthesia by producing

vasoconstriction at the site of injection (Epinephrine)

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Adverse effects

 Anxiety, fear, tension, headache, and tremor

 It can trigger cardiac arrhythmias, (if the patient is receiving

digoxin)

 Induce pulmonary edema

 May have enhanced cardiovascular actions in patients with

hyperthyroidism (dose must be reduced)
 Increases the release of endogenous stores of glucose
 In diabetic patients, dosages of insulin may have to be
increased

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Dopamine

 It is the immediate metabolic precursor of norepinephrine

 occurs naturally in the CNS as well as in the adrenal medulla

 Dopamine can activate α- and β-adrenergic receptors

 At higher doses, it causes vasoconstriction (α1 receptors)

 at lower doses, it stimulates β1 cardiac receptors

 In addition, D1 and D2 dopaminergic receptors occur in the

peripheral mesenteric and renal vascular beds, where binding
of dopamine produces vasodilation

 D2 receptors are also found on presynaptic adrenergic neurons

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 pharmacologic actions

Cardiovascular

 Exerts a stimulatory effect on the β1 receptors of the heart (positive

inotropic and chronotropic effects)

 Activates α1 receptors on the vasculature ( vasoconstriction)

Renal and visceral

 Dilates renal and splanchnic arterioles by activating dopaminergic

receptors (increases blood flow to the kidneys)

 clinically useful in the treatment of shock, in which significant

increases in sympathetic activity might compromise renal function

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Therapeutic uses

 Cardiogenic and septic shock

 It raises blood pressure by stimulating the β1 receptors on

the heart to increase cardiac output and α1 receptors on
blood vessels to increase total peripheral resistance

 It enhances perfusion to the kidney and splanchnic areas

enhances the GFR and causes diuresis

 Hypotension and severe heart failure ( in patients with low or

normal PVR and in patients who have oliguria)

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Adverse effects

 The same effects as sympathetic stimulation?

 Dopamine is rapidly metabolized by MAO or COMT, and its

adverse effects (nausea, hypertension, and arrhythmias) are,

therefore, short-lived

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Adrenergic antagonists (Sympatholytics)

 Also called adrenergic blockers

bind to adrenoceptors but do not trigger the usual

receptor-mediated intracellular effects

 These drugs act by either reversibly or irreversibly attaching to

the adrenoceptors

 thus preventing activation by endogenous catecholamines

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Alpha 1 (α1) adrenergic blocking agents

Prazosin

Terazosin

Doxazosin

Tamsulosin

Alfuzosin

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 Mechanism of action

 Are selective competitive blockers of the α1-receptors

Drugs that block α1- adrenoceptors profoundly affect blood

pressure

 blockade of these receptors reduces the sympathetic tone of

the blood vessels, resulting in decreased PVR.

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Therapeutic uses

 Treatment of hypertension

 Prazosin

 Terazosin

 Doxazosin

 An alternative to surgery in patients with BPH

 Tamsulosin

 Alfuzosin
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 Pharmacokinetics

 Metabolism leads to inactive products that are excreted in

urine

 except for those of doxazosin, which appear in feces

 Doxazosin is the longest acting of these drugs

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Adverse effects

 Dizziness, nasal congestion, headache, drowsiness

 Orthostatic hypotension

 The first dose of these drugs may produce an exaggerated

orthostatic hypotensive response that can result in syncope
(fainting)

 This action, termed a “first-dose” effect, may be minimized

by adjusting the first dose to one-third or one-fourth of the
normal dose and by giving the drug at bedtime

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  By blocking α1 receptors in the ejaculatory ducts and

impairing smooth muscle contraction, α1 antagonists may

cause inhibition of ejaculation and retrograde ejaculation

 “floppy iris syndrome”

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β -adrenergic blocking agents

 All of the clinically available β-blockers are competitive

antagonists

Nonselective β-blockers act at both β1 and β2 receptors

Cardioselective β-antagonists primarily block β1 receptors

 All β-blockers lower blood pressure

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Nonselective- ß antagonists

Propranolol

 Propranolol is the prototype β-adrenergic antagonist

 Sustained release preparations for once-a-day dosing are

available

Mechanism of action

 blocks both β1 and β2 receptors with equal affinity

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Actions

Cardiovascular

 diminishes cardiac output (negative inotropic and chronotropic

effects)

 During exercise or stress, when the sympathetic nervous system

is activated, β1-blockers attenuate the expected increase in
heart rate

 Cardiac output, workload, and oxygen consumption are

decreased by blockade of β1 receptors

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Peripheral vasoconstriction

 Nonselective blockade of β-receptors prevents β2-mediated

vasodilation in skeletal muscles, increasing peripheral vascular
resistance

 The reduction in cardiac output produced by all β-blockers

leads to decreased blood pressure, which triggers a reflex
peripheral vasoconstriction that is reflected in reduced blood
flow to the periphery

 In patients with hypertension, total peripheral resistance

returns to normal or decreases with long term use of
propranolol
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Bronchoconstriction

 Blocking β2 receptors in the lungs of susceptible patients

causes contraction of the bronchiolar smooth muscle

 This can precipitate an exacerbation in patients with chronic

obstructive pulmonary disease (COPD) or asthma

 Contraindicated in patients with COPD or asthma

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Disturbances in glucose metabolism

 Decreased glycogenolysis and decreased glucagon secretion

 If propranolol is given to a diabetic patient receiving insulin,

careful monitoring of blood glucose is essential

pronounced hypoglycemia may occur after insulin

injection

 Attenuate the normal physiologic response to hypoglycemia

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Therapeutic uses

Hypertension

 Lowers blood pressure in hypertension by several different

mechanisms of action

Decreased cardiac output is the primary mechanism

Inhibition of renin release from the kidney

decrease in total peripheral resistance with long-term use

Decreased sympathetic outflow from the CNS

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Angina pectoris

 Useful in the chronic management of stable angina

 Decreases the oxygen requirement of heart muscle

Effective in reducing chest pain on exertion that is common

in angina

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Myocardial infarction (MI)

 Have a protective effect on the myocardium

patients who have had one MI appear to be protected

against a second heart attack by prophylactic use of
propranolol

Administration of a β-blocker immediately following a

myocardial infarction reduces infarct size and hastens
recovery

 By blocking of the actions of circulating catecholamines,

which increase the oxygen demand in an already
ischemic heart muscle
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Migraine

 effective in reducing migraine episodes when used

prophylactically

due to its lipophilic nature that allows it to penetrate the

CNS

Hyperthyroidism

 It is effective in blunting the widespread sympathetic

stimulation that occurs in hyperthyroidism

 In acute hyperthyroidism (thyroid storm)

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Pharmacokinetics

Orally active

Subject to first-pass effect

only about 25% of an administered dose reaches the

circulation

The volume of distribution is quite large (4 L/kg)

the drug readily crosses the blood–brain barrier

Propranolol is extensively metabolized

Metabolites are excreted in the urine

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Adverse effects
Bronchoconstriction
Arrhythmias
Long-term treatment with a β antagonist leads to up-
regulation of the β-receptor
Treatment with β-blockers must never be stopped
abruptly because of the risk of precipitating cardiac
arrhythmias, which may be severe
 must be tappered for weeks
Sexual impairment
 β-blockers do not affect ejaculation or internal bladder
sphincter function (mediated through α-adrenergic activation)
 But some men do complain of impaired sexual activity??
The reasons for this are not clear and may be independent
of β receptor blockade
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Metabolic disturbances

 Decreased glycogenolysis and decreased glucagon secretion

Fasting hypoglycemia may occur

Perception of symptoms of hypoglycemia such as tremor,

tachycardia, and nervousness are blunted by β-blockers

CNS effects

 depression, dizziness, lethargy, fatigue, weakness, visual

disturbances, hallucinations, short-term memory loss,
emotional lability, vivid dreams (including nightmares)

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Drug interactions

 Drugs that interfere with, or inhibit, the metabolism of

propranolol, such as

cimetidine, fluoxetine, paroxetine, and ritonavir, may

potentiate its antihypertensive effects.

 Conversely, those that stimulate or induce its metabolism, such

as

barbiturates, phenytoin, and rifampin, can decrease its

effects.

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Selective β1-antagonists

 Acebutolol

 Atenolol

 Betaxolol

 Bisoprolol

 Esmolol

 Metoprolol

 Nebivolol

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 General pharmacology

 Drugs that preferentially block the β1 receptors

 minimize the unwanted bronchoconstriction ( β2 effect)

 Because these drugs have less effect on peripheral vascular

β2 receptors, coldness of extremities (Raynaud
phenomenon), a common side effect of β-blockers, is less
frequent

 This cardio-selectivity is most pronounced at low doses and is

lost at high doses

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Pharmacologic Actions

Lower blood pressure (in hypertension)

Increase exercise tolerance in angina

The cardioselective β-blockers have fewer effects on

pulmonary function

peripheral resistance

carbohydrate metabolism

In addition to its cardioselective β blockade, Nebivolol

releases nitric oxide from endothelial cells and causes
vasodilation
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Therapeutic uses

 Hypertensive patients with impaired pulmonary function

 First-line therapy for chronic stable angina

 Chronic heart failure (Bisoprolol and metoprolol)

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Parasympathetic nervous system

 Involved with maintaining homeostasis within the body

 It is required for life, since it maintains essential bodily

functions, such as digestion and elimination of wastes

 Usually acts to oppose or balance the actions of the

sympathetic division and generally predominates the

sympathetic system in “rest-and-digest” situations

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Cholinergic neuron

 A cholinergic neuron is a nerve cell which mainly uses

the neurotransmitter acetylcholine (ACh) to send its messages

 Many neurological systems are cholinergic

 The preganglionic fibers terminating in the adrenal medulla

 Preganglionic fibers (both parasympathetic and sympathetic)

 the postganglionic fibers of the parasympathetic division

 The postganglionic sympathetic division of sweat glands

 muscles of the somatic system and in CNS

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Cholinergic receptors

 Cholinergics stimulate the parasympathetic nervous system by

acting on cholinergic receptors

2 types of cholinergic receptors

1. Muscarinic - (M1, M2, M3, M4, M5 )

2. Nicotinic – (Neuromuscular and Ganglionic)

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Parasympathetic Responses of the body
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Cholinergic Agonists (parasympathomimetics)

 Acetylcholine

Mechanism of action

 act on cholinergic receptors to activate a tissue response by

stimulating parasympathetic NS

 All Cholinergic agonists mimic the effects of endogenous ACh

by binding directly to cholinoceptors (muscarinic or nicotinic)

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 Pharmacologic actions

 Cardiovascular

 Decrease in heart rate and cardiac output

 Decrease in blood pressure

Injection of ACh causes vasodilation and lowering of

blood pressure by an indirect mechanism of action

 In the gastrointestinal (GI) tract

 increases salivary secretion

 Stimulates intestinal secretions and motility

 It also enhances bronchiolar secretions

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  In the genitourinary tract

 Increases tone of the detrusor muscle (causing urination)

 In the eye

 ACh is involved in stimulation of ciliary muscle contraction

for near vision and in the constriction of the pupillae

sphincter muscle

– causing miosis (marked constriction of the pupil)

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Therapeutic use

 ACh (1% solution) is instilled into the anterior chamber of the eye

to produce miosis during ophthalmic surgery

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Bethanechol

Actions

 Directly stimulates muscarinic receptors

causing increased intestinal motility and tone

 stimulates the detrusor muscle of the bladder, whereas

sphincter muscles are relaxed

 These effects produce urination

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Therapeutic applications

 In urologic treatment

Stimulate the atonic bladder

– In postpartum or postoperative, nonobstructive urinary

retention

Neurogenic atony

Megacolon

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Adverse effects

 Sweating, salivation, flushing, decreased blood pressure,

nausea, abdominal pain, diarrhea, and bronchospasm

Atropine sulfate may be administered to overcome

severe cardiovascular or bronchoconstrictor responses

to this agent

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Carbachol (carbamylcholine)

 Profound effects on both the cardiovascular and GI systems

because of its ganglion-stimulating activity

 It can cause release of epinephrine from the adrenal

medulla by its nicotinic action

 Locally instilled into the eye, it mimics the effects of ACh,

 causing miosis

 spasm of accommodation in which the ciliary muscle of the

eye remains in a constant state of contraction

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Therapeutic uses

 Glaucoma

by causing pupillary contraction and a decrease in

intraocular pressure

Adverse effects

 At doses used ophthalmologically, little or no side effects occur

due to lack of systemic penetration (quaternary amine)

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Cholinergic antagonists (parasympatholytics)

Mechanism of action

 block muscarinic receptors

• causing inhibition of muscarinic functions

 Also block the few exceptional sympathetic neurons that are

cholinergic (those innervating the salivary and sweat glands)

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Atropine

 It is a tertiary amine belladonna alkaloid with a high affinity for

muscarinic receptors

Mechanism of action

 binds competitively & prevents ACh from binding to those sites

 Atropine acts both centrally and peripherally

 The greatest inhibitory effects are on bronchial tissue and

the secretion of sweat and saliva

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Pharmacologic actions

Eye

 Atropine blocks muscarinic activity in the eye

Mydriasis (dilation of the pupil)

Cycloplegia (paralysis of ciliary muscle of the eye)

 unresponsiveness to light

 inability to focus for near vision

 In patients with angle-closure glaucoma, intraocular pressure

may rise dangerously

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Gastrointestinal (GI)

 Atropine is probably the most potent antispasmodic drugs

available

Although gastric motility is reduced, hydrochloric acid

production is not significantly affected

 Not effective for the treatment of peptic ulcer

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Cardiovascular

 At low doses, the effect is a slight decrease in heart rate

From blockade of the M2 receptors on the inhibitory

prejunctional (or presynaptic) neurons, thus permitting

increased Ach release

 Higher doses of atropine cause a progressive increase in heart

rate by blocking the M1 receptors on the SA node

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Secretions

 Atropine blocks muscarinic receptors in the salivary glands

Producing dryness of the mouth (xerostomia)

 Sweat and lacrimal glands are similarly affected

 Inhibition of secretions by sweat glands can cause elevated

body temperature (can be dangerous in children & elderly)

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Therapeutic uses

Ophthalmic

 Topical atropine exerts both mydriatic and cycloplegic effects

This permits the measurement of refractive errors without

interference by the accommodative capacity of the eye

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Antispasmodic

 Atropine is used as an antispasmodic agent to relax the GI tract

Cardiovascular

 Used to treat bradycardia of varying etiologies

Antisecretory

 Used as an antisecretory agent to block secretions in the upper

and lower respiratory tracts prior to surgery

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Antidote for cholinergic agonists

 Organophosphate (insecticides, nerve gases) poisoning

 Overdose of physostigmine

 In some types of mushroom poisoning (certain mushrooms

contain cholinergic substances that block cholinesterases)

• The ability of atropine to enter the CNS is of particular

importance in treating central toxic effects of

anticholinesterases

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Pharmacokinetics

 Atropine is readily absorbed after oral administration

 Partially metabolized by the liver

 eliminated primarily in urine

 It has a half-life of about 4 hours

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Adverse effects

 Dry mouth

 blurred vision & “sandy eyes”

 Tachycardia

 Urinary retention & constipation

 Restlessness, confusion, hallucinations, delirium, & depression

 Collapse of the circulatory and respiratory systems

The drug may be dangerous in children, because they are

sensitive to its effects, particularly to rapid increases in body
temperature that it may elicit
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Quiz 1
1. Write the two primary neurotransmitters in the ANS?
2. A drug used as an alternative to surgery in patients with BPH
A. Prazosin
B. Tamsulosin
3. The drug of choice for the treatment of anaphylactic shock?
A. Dopamine
B. Epinephrine
4. The drug of choice for the treatment of cardiogenic shock?
A. Dopamine
B. Epinephrine

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