mech: inc IP3+DAG and [Ca++]

action: activates/stims myenteric plexus

mech: opens K+ channels / dec cAMP, dec Ca++ 

action: dec HR and contraction / inhibit NE release from symp nerve terminals

mech: inc IP3+DAG and [Ca++]

action: 

 - contracts circular muscle (pupil constric)

 - contracts ciliary muscle (near focus)

 - contracts brochiolar muscle, GI SM, uterine muscle, blatter detrusor 

 - relaxes vasc muslce (via NO from endo)

 - stims secretions of GI tract, eccrine sweat glands, tear glands, salivary glands, pancreatic fluids, liver bile

Nn: neuronal, located in symp and para postganglionic cells as well as in cortical and subcortical nuclei in the brain

Nm: membranes of skeletal muscles

• trade: 
• half-life:
• MoA: stims Nn receptors
• Elim:
• Rx: withdrawal symtpoms of smoking cessation
• tox: 
• notes: bc nic recs on post-gang cells of both SNS and PNS, can activate both systems simultaneously

• trade: 
• half-life: 
• MoA: Nm blocker. depolarization block
• Elim: butyrl cholinesterase
• Rx: muslce relaxant during intubation or electroconvulsive shock therapy 
• tox: 
• contras: fam history of familial hyperthermia, skeletal muscle myopathies

• trade: 
• half-life: 150sec (RAPID!)
• MoA: binds M and N receptors
• Elim: AchE
• Rx: none--not used clinically.
• tox: 
• note: quaternary nitrogen analog

• half-life: short, but longer than Ach
• MoA: Musc agonist
• Elim: AchE
• Rx: to Dx bronchial hyperactivity in pts suspected of having asthma
• tox: bronchiolar constriction
• contras: pts given B-blockers
• note: quaternary nitrogen analog (no xBBB)

• half-life: long
• MoA: nic and musc agonist
• Elim: AchE (but resistant)
• Rx: miotic agent in ocular surgery, to reduce pressure following ocular surgery
• tox: xs nic and musc activation
• notes: quaternary nitrogen analog

• trade: 
• half-life: 
• MoA: musc agonist (esp GI and urinary bladder)--very little M2 activity. LACK of nic activity*
• Elim: 
• Rx: treat post-op or post-partum urinary retention, treat bladder atony
• tox: bradycardia
• contra: peptic ulcer, asthma, bradycardia
• notes: quaternary nitrogen analog

• half-life: ~1hr
• MoA: pure musc agonist
• Elim: 
• Rx: narrow angle glaucoma, dry mouth (due to head and neck radiotherapy or Sjogren's syndrome)
• tox: 
• notes: "pile guacemole (glaucoma) in his dry mouth"
• also, crosses BBB
• NATURALLY OCCURING TERTIARRY AMINE

• half-life:
• MoA: reversible cholinesterase (AchE) inhibitor!
• Elim:
• Rx: mysasthenia gravis, reverse neuromuscular blockade
• tox: xs Ach action at musc and nic sites
• contras: intestinal obstruction
• notes: poorly xBBB

• half-life: ~10min (rapid onset, short duration of action...good for diag)
• MoA: reversible AchE inhibitor
• Elim: 
• Rx: diag of myasthenia gravis vs cholinergic crisis, reversal of neuromusc block
• tox: bradycardia
• contras: mechanical block of intestine and urinary tract

• half-life: up to 2hrs
• MoA: reverisble AchE inhibitor
• Elim: 
• Rx: counteract delirium associated w xs Ach activation--antidote for Musc antagonist poisoning
• tox: xs Ach at musc and nic sites
• contras: asthma, cardiac insufficiency, gut obstruction
• notes: readily xBBB

• half-life: 70hrs (long!)
• MoA: reversible AchE inhibitor
• Elim: 
• Rx: Alzheimer's Dx
• tox: 
• contras: 

Diarrhea

Urinary frequency and incontinence

Miosis

Bradycardia

Bronchorrea/Bronchoconstriction

Emesis

Lacrimation

Laxation

Salivation

• half-life: 75min
• MoA: peripheral AchE reactivator
• Elim: 
• Rx: respiratory muscle weakness in organophosphate poisoning
• tox: 
• contras: 

1. mechanical VENTILATION to counter effects on neurmusc junction

2. SUCTION of oral secretions

3. ATROPINE to protect from systemic muscarinic effects

4. pralidoximine chloride (2-PAM)

• half-life: very long
• MoA: irreversible AchE inhibitor
• Elim: 
• Rx: produce long-term miosis in treatment of open angle glaucoma
• tox: 
• contras: 

• half-life: 
• MoA: muscarinic antagonist
• Elim: 
• Rx: 
• 1. to allay urg and freq of micturition
• 2. relieve hypermotility of colon and hypertonicity of SI
• 3. treatment of AchE inhibitor induced poisoning
• 4. induce mydriasis and cycloplegia (paralysis of ciliary muscle)
• 5. reverse bradycardia of vagal origin
• tox: 
• contras: 

• half-life: 
• MoA: muscarinic antagonist
• Elim: 
• Rx: motion sickness, anti-salilgogue (to minimize secretions) in surgery
• tox: 
• contras: narrow angle glaucoma

• half-life: 
• MoA: muscarinic antagonist
• Elim: 
• Rx: to prevent overstim of gut during reversal of neuromusclular blockade
• tox: 
• contras: