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CHOLINERGIC AGONISTS
Agonist INITIATES A CHOLINERGIC RESPONSE
A. Direct Acting
1. Acetylcholine
2. Bethanecol
3. Carbachol
4. Pilocarpine
Oral: treatment of decreased salivation accompanying

4.

Pyridostigmine and ambenonium

Chronic management of MG
Duration of action are intermediate (3-6, 4-8 hours)

5.

Tacrine, donzepezil, rivastigmine, galantamine

Alzheimers delay progression
Adverse effect: GI distress

head and neck irradiation

B. Indirect Acting (ACETYLCHOLINESTERASE INHIBITOR);
Reversible
1.

Edrophonium
Used in diagnosis of MG: which is an autoimmune
disease caused by antibodies to the nicotinic receptor
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at NMJs
There is degradation resulting in fewer receptors

available for interaction with neurotransmitters

IV: rapid increase in muscle strength: may provoke

cholinergic crisis:
o Atropine is the antidote
Used in differentiating cholinergic and myasthenic
crisis: both are marked by severe muscle weakness

Symptomatic MG treatment
Adverse effects: generalized cholinergic stimulation

C. Indirect Acting: Anticholinesterases (Irreversible)

1. Echothiopate
Open angle glaucoma
D. Organophosphate toxicity
Manifested as muscarinic and nicotinic s/sx
Nicotinic effects:
o Hypertension
o Tachycardia
o Pallor
o Mydriasis (dilation)
Management:
o Pralidoxime reactivate inhibited AChE
o Atropine prevent muscarinic effects
o Diazepam
o General supportive measures

and difficulty breathing

o Myasthenic crisis: worsening of condition

Respiratory distress

Dysphagia

Dysarthria

Ptosis, diplopia

Prominent muscle weakness

Management:

Intubation, NGT

ABGs, Serum electrolytes,

I/O, daily weight

CPPT, suctioning
Avoid sedatives and
tranquilizers aggravate
hypoxia and hypercapnea
further respi and cardiac

CHOLINERGIC ANTAGONISTS

depression
Cholinergic crisis: overdose of

parasympatholytics, anticholinergic drugs)

anticholinesterase drugs
A.
2.

3.

Physostigmine
Increase intestinal and bladder motility
Ophthalmic: miosis and spasms of accommodation
Used in overdose of anticholinergics: atropine,
TCA,phenothiazines
Neostigmine

Also known as: cholinergic blockers,

Antimuscarinic Agents
Selectively blocks muscarinic receptors: action of
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1.

sympathetic stimulation are unopposed

Inhibits all muscarinic functions

Atropine

2.

Persistent dilation of the pupil, unresponsiveness to

light, cyclopegia (inability to focus for near vision)
o Tx: narrow angle glaucoma
o Phenylephrine is favored over atropine
Reduced GI motility, but Hcl production is not
Used in enuresis among children
Produces xerostomia
Antidote for cholinergic agonists
Side effects:
o Dry mouth
o Blurred vision
o Sandy eyes
o Tachycardia
o Urinary retention
o Constipation
CNS effects:
o Restlessness
o Confusion
o Delirum
o Hallucination
Physostigmine overcome atropine toxicity

Ipratropium and tiotropium

Bronchodilators
Tiotropium: once daily vs. ipra (4x)
Inhalation

4.

Tropicamide and cyclopentolate

Ophthalmic solution of mydriasis and cyclopegia

5.

Benztropne and trihexyphenidyl

Adjuncts to antiparkinsonian agents

B.

C.

Darifenacin, fesoterodine, oxybutynin, solifenacin,

tolterodine, and trospium chloride
Treat overactive urinary bladder disease
Ganglionic Blockers
1. Nicotine
2. Mecamylamine
Neuromuscular Blockers
Interfere with transmission of Efferent impulses to
skeletal muscles; muscle relaxant adjuvants

1.

o
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Nonpolarizing Agents
Mechanism of action:

excitatory)
High doses: complete blockade, no direct

electrical stimulation
Action: FIRST TO LAST AFFECTED:
o Face and eyes muscles small rapidly
contracting
o Fingers
o Limbs
o Neck and trunk
o ICS
o Diaphragm
Reversal: recovery
Mode: IV only, terminated by redistribution not
metabolized
AE: generally safe with minimal SE
Drug interactions:
o Halothane decrease the effect
o Calcium channel blockers and
aminoglycoside antibiotics: increase the
a.

and blocking short term memory

More effective prophylactially
Adjunct in anesthetic procedures

3.

Low doses: Prevent binding of Ach inhibits

muscular contraction (remember that ACh is

Scopolamine
Anti-motion sickness drug
May produce euphoria abuse
Indications: limited to prevention of motion sickness
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6.

effect
Cistracurium
i. Spontaeously degrades in plasma
ii. Dose need not be reduced in renal
iii.

failure
Used in MOSF metabolism is
independent of renal and hepatic

b.
c.
d.
e.
2.

function
Pancuronium vagolytic (increase HR)
Rocuronium
Tubocurarine
Vecoronium

Polarizing Agents
a. Succinylcholine
i. Common SE: post-op muscle pain
ii. Hyperkalemia and increased IOP and

iv.

intragastric pressure may occur

May trigger malignant hyperthermia
1. Cool patient
2. Administer dantrolene
Indicated if rapid intubation is necessary,

v.

esp if patient has gastric contents

Rapid onset, brief duration, usually given

iii.

continuous infusion

ADRENERGIC AGONISTS

A.

Catecholamines:
1. Epinephrine
2. Norepinephrine
3. Isoproterenol
4. Dopamine
5.

Characteristics of catecholamines:
1.
2.
3.
B.
1.
2.
3.

High potency
Rapid inactivation (IV, never PO)
Do not penetrate CNS

Noncatecholamines
Have longer half-lives
Phenylepinephrine
Ephedrine
Amphetamine