para

Where do cholinergic synapses occur?

All postganglionic parasympathetic nerves, sympathetic nerves to sweat glands, autonomic ganglia, adrenal medulla, somatic motor nerves and CNS

What is the first neurotransmitter discovered?

Acetylcholine

What are the two types of cholinesterase?

AChE and BuChE

Where is AChE located?

Cholinergic neurons, ganglia, RBCs and NMJ

Where is BuChE located?

Liver, plasma and glial cells

Which cholinesterase is found in serum?

BuChE (pseudocholinesterase)

Which cholinesterase metabolizes succinylcholine?

BuChE

Location of Nn receptors?

Autonomic ganglia and adrenal medulla

Location of Nm receptors?

Skeletal muscle

Function of Nn receptors?

Ganglia stimulation and adrenaline release

Function of Nm receptors?

Skeletal muscle contraction

Location of M1 receptors?

Glands and CNS

Location of M2 receptors?

Heart and CNS

Location of M3 receptors?

Glands and smooth muscles

Why is acetylcholine not used therapeutically?

Rapidly destroyed by cholinesterase

Methacholine receptor selectivity?

Muscarinic only

Is methacholine hydrolyzed by cholinesterase?

Yes

Methacholine therapeutic use?

Paroxysmal atrial tachycardia

Carbachol receptor selectivity?

Muscarinic and Nicotinic

Is carbachol hydrolyzed by cholinesterase?

No

Carbachol therapeutic use?

Eye drops for glaucoma

Bethanechol receptor selectivity?

Muscarinic only

Bethanechol therapeutic uses?

Non-obstructive paralytic ileus and urinary retention

Bethanechol is especially useful in?

Postpartum and post-operative urinary retention

Pilocarpine therapeutic uses?

Glaucoma, urinary retention, paralytic ileus and Sjögren syndrome

Cevimeline therapeutic use?

Xerostomia in Sjögren syndrome

What is Sjögren syndrome?

Autoimmune disease causing chronic dryness

Most common symptom of Sjögren syndrome?

Chronic dryness throughout the body

Side effects of muscarinic agonists mnemonic?

DUMBELS

Reversible anticholinesterases act by?

Carbamylation

Irreversible anticholinesterases act by?

Phosphorylation

Examples of reversible anticholinesterases?

Physostigmine, Neostigmine, Pyridostigmine, Edrophonium, Donepezil, Rivastigmine

Examples of irreversible anticholinesterases?

Organophosphates

Physostigmine source?

Plant origin

Physostigmine chemistry?

Tertiary ammonium compound

Does physostigmine cross BBB?

Yes

Physostigmine therapeutic uses?

Glaucoma and atropine poisoning

Neostigmine source?

Synthetic

Neostigmine chemistry?

Quaternary ammonium compound

Does neostigmine cross BBB?

No

Neostigmine therapeutic uses?

Myasthenia gravis, urinary retention, paralytic ileus, curare poisoning and reversal of non-depolarizing blockers

Why is atropine given with neostigmine?

To block muscarinic side effects

Pyridostigmine chemistry?

Quaternary ammonium compound

Drug of choice for Myasthenia Gravis?

Pyridostigmine

Pyridostigmine duration?

Long acting

First drug used for Alzheimer disease?

Tacrine

Why was Tacrine replaced?

Hepatotoxicity

Drugs used in Alzheimer disease?

Donepezil, Rivastigmine and Galantamine

Edrophonium class?

Reversible anticholinesterase

Edrophonium duration?

Rapid onset and short duration

Drug used in Tensilon test?

Edrophonium

Edrophonium differentiates between?

Myasthenic crisis and cholinergic crisis

Curare mechanism?

Blocks nicotinic receptors at NMJ and autonomic ganglia

Curare antidote?

Cholinesterase inhibitors

What is Myasthenia Gravis?

Autoimmune disease against nicotinic receptors

Main symptom of Myasthenia Gravis?

Muscle weakness

Organophosphates mechanism?

Irreversible inhibition of acetylcholinesterase

What is aging?

Enzyme-organophosphate complex becomes resistant to hydrolysis

Antidote of organophosphate poisoning?

Pralidoxime (PAM)

When is PAM effective?

Before aging occurs

Life-saving drug in organophosphate poisoning?

Atropine

Examples of organophosphate insecticides?

Parathion and Malathion

Examples of nerve gases?

Sarin, Soman and Tabun

Cause of death in organophosphate poisoning?

Respiratory failure

Signs of atropinization?

Mydriasis, tachycardia and dryness

Anticonvulsant used in organophosphate poisoning?

Diazepam

Atropine classification?

Competitive non-selective muscarinic blocker

Does atropine cross BBB?

Yes

Main cardiac effect of atropine?

Tachycardia

Effect of atropine on bronchi?

Bronchodilation

Effect of atropine on bladder?

Detrusor relaxation and sphincter contraction

Effect of atropine on eye?

Mydriasis and cycloplegia

Atropine uses in bradycardia?

IV for symptomatic bradycardia

Atropine use in poisoning?

Antidote for organophosphate poisoning

Atropine eye use?

Fundus examination

Atropine adverse effects?

Dry mouth, constipation, urinary retention, tachycardia and glaucoma

Contraindication of atropine?

Glaucoma

Atropine toxicity triad?

Mydriasis, red hot dry skin and CNS manifestations

Antidote of atropine toxicity?

Physostigmine

Drug of choice for motion sickness?

Hyoscine (Scopolamine)

Main CNS effect of hyoscine?

Sedation and amnesia

Why is hyoscine preferred as preanesthetic medication?

Sedation, amnesia and antiemetic effect

How long does hyoscine patch work?

Up to 3 days

Use of glycopyrrolate?

Preanesthetic medication

Selective M1 blockers?

Pirenzepine and Telenzepine

Short acting anti-asthmatic antimuscarinic?

Ipratropium

Long acting anti-asthmatic antimuscarinic?

Tiotropium

Advantage of ipratropium and tiotropium?

Local inhaled action with minimal CNS effects

Anti-urinary incontinence drugs?

Oxybutynin, Tolterodine, Darifenacin and Solifenacin

These urinary drugs are selective for which receptor?

M3 receptor

Anti-parkinsonism antimuscarinic drugs?

Benztropine and Trihexyphenidyl

Ganglion stimulating drugs?

Nicotine and Varenicline

Varenicline mechanism?

Partial Nn agonist

Varenicline use?

Smoking cessation

Varenicline side effects?

Nausea, headache, insomnia, depression and suicidal ideation

Depolarizing ganglion blocker?

Large dose nicotine

Non-depolarizing ganglion blocker?

Trimethaphan

Use of Trimethaphan?

Hypertensive emergency

Neuromuscular blockers act on which receptor?

Nm receptor

Use of neuromuscular blockers?

Muscle relaxation during surgery and intubation