Pharm2 Cholinomimetics
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| Direct Muscarinic Agonists | 1.Acytelcholine.
2.Methacholine.
3.Bethanechol.
4.Pilocarpine.
5.Carbachol.
6.Cevimeline.
7.Muscarine.
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| Adverse effects of direct Muscarinic Agonists | 1.Inc Salivation.
2.Inc Sweating.
3.Intestinal cramps.
4.Aggravate Ulcer.
5.VD/Hypotension (Endothelial NO).
6.Bradycardia or reflex tachycardia (M2).
7.Asthma.
8.Near vision (lense rounding).
9.Miosis.
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| Direct Muscarinic Agonists: Acetylcholine & Methacoline | Mech of action: Directly binds to M receptors.
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| Direct Muscarinic Agonists: Pilocarpine | 1.Mech of action: Direct M agonist causing salivation, Inc aq humour outflow/drainage for Open & narrow angle glaucoma.
2.Oral, Topical-EYE.
3.Used to treat Open & Narrow Angle glaucoma, Sjogren's syndrome, radiation induced dry mouth.
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| What is the only drug used to treat NARROW angle Glaucoma (all others are for open angle)? | Pilocarpine
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| How does Pilocarpine affect Open angle glaucoma differently from Narrow angle glaucoma | OAG-Contracts ciliary m.: pulls on trabecular meshwork: open holes: Inc outflow of aq humor
NAG-contract the iris sphincter smooth m.: induce miosis: pulls the iris away from the trabecular meshwork: Inc outflow of aq humor: dec IOP
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| Direct Muscarinic Agonists: Bethanechol | 1.Mech of action: directly activates M receptors.
2.Used to treat Post-op abdominal distention & urinary retention, Neurogenic atony of the bladder w/o retention.
**used to treat NONOBSTRUCTIVE symptoms.
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| Direct Muscarinic Agonists: Carbachol | 1.Mech of action: Directly M agonist that contracts ciliary muscles Inc outflow/drainage of aq humour.
2.used as a 2nd line of defense after Pilocarpine for OAG.
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| Direct Muscarinic Agonists: Cevimeline | 1.Mech of action: Direct M agonist selective on salivary glands.
2.Bioav: longer lasting salivation effect (4-6hrs).
3.Used to treat Sjogren's syndrome (newer than Pilocarpine)
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| Direct Muscarinic Agonists: Muscarine | 1.Mech of action: direct M agonist.
2.From: Mushrooms.
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| Problems with ACh as a drug? | 1.Very short half life.
2.Activates N & M receptors.
3.TOO MANY SIDE EFFECTS.
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| What M agonist would be best to treat Urinary bladder and GI issues? | Bethanechol
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| Would Bethanechol be good to treat BPH? | NO!! it is and OBSTRUCTIVE urinary bladder w/ retention.
**Bethanechol only affects NONOBSTRUCTIVE.
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| What is Sjogren's Syndrome? | Autoimmune disease attacking salivary and tear glands.
**Treat with:
1.Pilocarpine,
2.Cevimeline (longer lasting and fewer side effects).
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