Pharmacology

Mechanism: Inhibits exocytosis of ACh

Indications: (cervical sytonia, strabismus, blepharospasm, spasticity, glabellar frown lines) (lower esophageal spasms) (hyperhidrosis)

Adverse Effects: Injection site reaction, weakness of injected muscle and adjacent muscles

Other: lasts 3-4 months

nAChR agonist

Mechanism: stimulates nAChRs

Indications: drug of abuse

Adverse Effects: increase BP, HR, CNS effects

• 1. D-tubocurarine
• 2. Succinylcholine

Mechanism: blocks NM receptors at NMJ (SKM paralysis)

Indications: during surgery (SKM relaxation)

Adverse Effects: produces significant N_N blockade, allergic reactions (histamine release)

Other: paralysis produced by competitive agents and can be reversed by anti-ChE, seldom used clinically

Mechanism: N_M receptor agonist, but produces persistent depolarization --> SKM paralysis

Indications: surgery (SKM relaxation)

Other: rapidly hydrolyzed by BuChE (short duration of action)

Competitive and non-competitive

Adverse Effects: postural hypotension, constipation, urinary retention, xerostomia

Other: formerly used to tx HTN

• 1. Choline Esters (bethanechol)
• 2. Natural (muscarine)
• 3. Alkaloids (Pilocarpine)

Mechanism: stimulate mAChRs

Indications: postoperative ileus, urinary retention

Adverse Effects: GI side effects (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation

Mechanism: stimulate mAChR

Indications: Xerostomia due to damage to salivary glands, glaucoma

Adverse Effects: Adverse Effects: GI side effects (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation

• 1. Atropine
• 2. Scopolamine
• 3. Oxybutynin
• 4. Tolterodine
• 5. Ipratropium

Mechanism: blocks mAChRs

Indications: bradycardia, AV block

Side Effects: xerostomia, constipation, urinary retention, confusion

Mechanism: block mAChRs

Indications: motion sickness

Side Effects: xerostomia, constipation, urinary retention, confusion

Other: prominant CNS effects

Mechanism: block mAChRs

Indications: overactive bladder, enuresis, neurogenic bladder

Side Effects: xerostomia, constipation, urinary retention, confusion

Mechanism: block mAChRs

Indications: COPD

Side Effects: xerostomia, constipation, urinary retention, confusion

• 1. noncovalent (Donepezil)
• 2. Carbamoylating (Physostigmine)
• 3. Phosphorylating (Echothiophate, Malathion)

Mechanism: interacts noncovalently with active site of AChE

Indications: Alzheimer's

Side Effects: GI (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation

Mechanism: carbamoylates the active site of AChE, blocking enzyme activity

Indications: Glaucoma, Toxicology

Side Effects: GI (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation (minimized by topical application)

Mechanism: phosphorylates the active site of AChE, blokcing enzyme activity

Indications: Glaucoma

Side Effects: GI (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation

Other: only used for Pts who have not responded to other therapies

Mechanism: phosphorylates the active site of AChE, blocking activity of the enzyme

Indications: insecticides

Side Effects: GI (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation

Pralidoxime

Mechanism: Nucleophilic attack on AChE (phosphorylated), regenerates active enzyme

Indications: toxicology

Other: not effective if phosphorylated AChE has aged