Cholinergic & Anticholinergic

Drugs
Cholinergic drugs (cholinomimetics)
Drugs that produce actions similar to cholinergic
system stimulation.

Cholinergic receptor blockers(anticholinergic)

Drugs that block cholinergic receptors thus prevent
actions of cholinomimetics.

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Cholinergic & anticholinergic actions
Cholinergic actions Anticholinergic actions
Eye
Miosis Mydriasis

Heart
bradycardia ( heart rate )
Urinary bladder
Contraction of muscles
Relaxation of sphincter
Tachycardia ( heart rate)
force of contraction
Relaxation of muscles
contraction of sphincter

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 Cholinergic actions Anticholinergic actions
Exocrine glands
Increase of sweat, saliva, Decrease of all secretion
lachrymal, bronchial,
intestinal secretions
GIT
peristalsis peristalsis
secretion secretion
relaxation of sphincter Contraction of sphincter

Lung
1. Constriction of bronchial 1. Relaxation of bronchial
smooth muscles muscles
2. 4Increase bronchial secretion 2. Decrease secretion
 Cholinomimetics = Parasympathomimetics
Types
1. Direct cholinomimetics
Act by direct stimulation of cholinergic receptors.
2. Indirect cholinomimetics
They act indirectly by inhibiting acetylcholinesterase
thus amplify the action of endogenous acetylcholine

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 Cholinomimetic drugs
(Cholinergic drugs)
1) Direct cholinomimetics
Naturally occurring alkaloids e.g. Pilocarpine
Synthetic choline esters
Acetylcholine
Methacholine
Carbachol
Bethanechol

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2. Indirect acting cholinomimetics
Alcohol (short acting)- reversible
Edrophonium

Carbamates esters (intermediate) -

reversible
Physostigmine, Neostigmine

Phosphates (very long acting)-

irreversible
Ecothiophate
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Paroxysmal atrial tachycardia
A period of very rapid and regular heart beats that begins and
ends abruptly. The heart rate is usually between 160 and 200
beats per minute.

paralytic ileus
a decrease in or absence of intestinal peristalsis. It may occur
after abdominal surgery or peritoneal injury

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Uses of cholinomimetics
1. Treatment of galucoma
(Pilocarpine- carbachol - physostigmine).
2. Postoperative paralytic ileus & urinary
retention
(bethanechol carbachol neostigmine).
3. Treatment of myasthenia gravis
(neostigmine).
4. Antimuscarinic drug intoxication

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 Anticholinergic Drugs
(Muscarinic blockers)
e.g atropine , hyoscine
Uses of antimuscarinics
Bronchial asthma
Parkinsonism
Ophthalmoscope examination of retina
Peptic ulcer (Pirenzepine).
Antiemetics, motion sickness (Hyoscine).
Antispasmodic for intestinal and renal colics
Traveller 's diarrhea

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 Adverse drug effects
Cholinergic actions Anticholinergic actions
Nausea Dry mouth
Vomiting & diarrhea Blurred vision
Salivation Tachycardia
Bronchconstriction Hot flushed skin
Agitation & confusion
Increase in body temp
Constipation
Urinary retention

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 Adrenergic receptors
Adrenergic
Receptors

Alpha Beta
Receptors Receptors

Beta 1 Beta 2
Receptors Receptors

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 Alpha-adrenergic Receptors
Found predominantly on smooth muscle
membrane.

When stimulated by NE or EPI produce

contraction.

Produces vasoconstriction of most blood

vessels.
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 Beta 2
Receptors

Beta 1
Receptors

Found on smooth
Found on smooth muscle Found on smooth
muscle in the
of blood vessels supplying muscle in the heart
bronchial tree.
skeletal muscle and the heart.

Increase heart rate and

Bronchodilation. force of contraction.
Vasodilatation.

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 Adrenergic drugs
(sympathomimetics)
Sympathomimetic
Drugs

Alpha-adrenergic Beta- adrenergic

Selective Beta 1 Selective Beta 2

Adrenergic. Adrenergic.

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 Alpha-adrenergic Drugs
Clinical Indications

Hypotensive states

Decongestion

Pupillary dilation

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 Alpha-adrenergic Drugs
Adverse Effects

Hypertensive crisis

Cerebral hemorrhage

Cardiac arrhythmias

Irritation of the nasal sinuses or eye.

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 Alpha-adrenergic Drugs

Drug Main Use

Epinephrine To increase BP

Norepinephrine To increase BP

Pseudoephedrine Nasal decongestion

Tetrahydrozoline Ophthalmic decongestion

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 Beta-adrenergic Drugs
Stimulation of the heart

Bronchodilation

Relaxes uterine smooth muscle

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 Beta-adrenergic Drugs

Drugs Classification Main Use

Epinephrine Alpha, Beta-1 and Vasopressor, Cardiac stimulant,

Beta-2 bronchodilator.
Isoproterenol Beta-1 and Beta-2 Cardiac stimulant,
bronchodilator.

Albuterol Beta-2 Bronchodilator.

Ritodrine Beta-2 Arrest preterm labor.

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 Epinephrine
Use in combination with local anesthetics.
Used as a cardiac stimulant in emergencies.
Use in the treatment of asthma.
Adverse Effects
CNS stimulation tremor, restlessness, anxiety
(beta effect)
Over-stimulation of the heart (beta 1 effect)
Lower blood pressure (beta 2 effect)

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 Dopamine
Neurotransmitter in the brain.
Precursor in the synthesis of NE
Stimulates dopaminergic, beta-1 and
alpha-receptors.
Use as a drug.
Dobutamine similar to dopamine but with
more Beta-1 effect.

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 Dopamine
DOPAMINE RECEPTORS EFFECTS
DOSE STIMULATED

Low dose Stimulate dopaminergic Increased renal blood flow and

receptors in the renal and vasodilatation.
mesenteric blood vessels.

Moderate dose Stimulates beta-1 receptors Increase myocardial

in the heart. contractility.

Higher dose Stimulate alpha-receptors Produces vasoconstriction.

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 Alpha-adrenergic blocking drugs
Binds to Alpha receptors
Antagonizes the effects of NE and EPI
Leads to a decrease in sympathetic response
Resulting in vasodilatation and thus decrease in BP.
Clinical Indications
Treatment of hypertension.
Vasodilator in treatment of Raynauds disease(vasospastic
disorder causing discoloration of the fingers, toes).
Diagnosis of Pheochromocytoma(neuroendocrine tumor
of the medulla of the adrenal glands).

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Alpha-adrenergic blocking drugs
Adverse Effects
Constriction of pupils
Increased GI activity
Nasal congestion
Reflex tachycardia ( if BP is lowered too much).

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 Alpha-adrenergic blocking drugs

Drugs Main Use

Doxazosin Treatment of Hypertension

Prazosin Treatment of Hypertension

Phentolamine Diagnosis of pheochromocytoma.

Treatment of vascular disease.

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 Beta-adrenergic blocking drugs
Binds to beta receptors
Antagonizes the effects of NE and EPI
Leads to a decrease in sympathetic response.
Resulting in decrease heart rate and force of
contraction.
Beta-blocking
Drugs

Non-selective Selective Beta-1

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 Beta-adrenergic blocking drugs
Nonselective Blockers Main Use

Labetalol Hypertension

Nadolol Hypertension, Angina Pectoris

Pindolol Hypertension

Propanolol Hypertension, Angina Pectoris,

arrhythmhias, migraine

Timolol Hypertension, post myocardial

infarction.
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 Beta-adrenergic blocking drugs
Selective Blockers Main Use

Acebutolol Hypertension, ventricular

arrhythmias.
Atenolol Hypertension, Angina Pectoris

Bisoprolol Hypertension

Esmolol Supraventricular tachycardia

Metoprolol Hypertension, Angina Pectoris

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 Propranolol
Decrease heart rate
Decrease force of contraction
Decrease rate of conduction
Resulting decrease in effort and work of the heart causes a
decrease in oxygen consumption.
Oral and iv preparation
Drug is carried directly to the liver by the portal system.
Significant first pass metabolism.
Lipid soluble and passes into the brain.
Causes CNS sedation, depression and decreased central
sympathetic activity.

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 Propranolol
Used in the treatment of angina, and various
cardiac arrhythmia.

Adverse effects include nausea, vomiting and

diarrhea, bradycardia with resulting reduced
cardiac function, bronchoconstriction.

Most serious drug interactions involve therapy of

beta blockers with other drugs that decrease
cardiac function .

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 Adrenergic neuronal blockers
Drugs that interfere with the formation and or
storage of NE
Alpha-methyl dopa
Reserpine
Guanethidine

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 Adrenergic neuronal blockers

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 Adrenergic neuronal blockers

Drugs Mechanism of Action Main Use

Alpha-methyl dopa Blocks formation of Treatment of

Dopamine hypertension

Reserpine Depletes NE storage Treatment of

granule hypertension

Guanethidine Block release of NE Treatment of

and depletes NE hypertension
storage granule

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