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Pharm Exam 1 (Cholinergics and Anti-Cholinergics)

Terms in this set (23)

Succinylcholine
Depolarizing neuromuscular blocker-
receptor selectivity- nicotinic receptor agonist
mechanisms-competes w/ ACh for nicotinic receptors to mimic ACh and depolarize motor end plate
therapeutic uses- skeletal muscle relaxant (IV)
side effects- Malignant hyperthermia (uncontrolled calcium release from SR in skeletal muscle)
Varenicline (Chantix)
receptor selectivity -Patrial agonist at a4β2 neuronal nicotinic receptors
mechanisms-High affinity; "competition" for nicotine, reduced pharmacologic reward
therapeutic uses- smoking cessation
side effects- vivid abnormal dreams, insomnia, constipation, boxed warning removed for psych & cardiovascular
Bupropion (Zyban; Wellbutrin SR)
receptor selectivity -non-seratonergic anti depressant, inhibits reuptake of dopamine (primary) and NE
mechanisms- increases NE, increased DA (urges)
therapeutic effect- smoking cessation 2nd line, anti-depressant
side effects - lowers seizure threshold, weight loss, agitation, insomnia, dry mouth, tachycardia
Acetylcholine (endogenous)
receptor selectivity- muscarinic cardiac (M2) , smooth muscle (M3) and some nicotinic
mechanism-
direct agonist- RELAX, lowers HR/CV, vasodilatio
Therapeutic effect- tachycardia, hypertension (agonist
side effects-
Methacholine
receptor selectivity- smooth muscle in bronchi (M3)
mechanisms-
agonist- CONTRACT broncoconstriction
Therapeutic effect-
asthma diagnosis (agonist)
side effects-
Carbachol (Miostat)
receptor selectivity- smooth muscle in ciliary eye muscle (M3)
mechanism-
agonist- CONTRACT miosis to drain aqueous humor
therapeutic effects-
glaucoma (agonist)
side effects-
Cevimeline (Evoxac)
receptor selectivity- muscarinic receptors in glands (M1/M3)
mechanism-
agonist- increase secretions salivary glands
therapeutic effects-
xerostomia Sjogren (agonist)
side effects-
Bethanechol (Urecholine)
receptor selectivity- smooth muscle muscarinic (M3)
mechanism-
agonist- CONTRACT increase GI motility
therapeutic effects-
Urinary retention, Gastric Atony (agonist)
side effects-
Pilocarpine (Pilocar)
receptor selectivity- muscarinic receptors in glands (M1/M3)
mechanism-
agonist- increase secretions/ CONTRACT miosis AH drains
therapeutic effects-
xerostomia Sjogren's, glaucoma (agonist)
side effects-
(Alzheimers AChIs)
Indirect Muscarinic Agonists
Tacrine
Rivastagmine
Galantamine
Donepezil
receptor selectivity- Nicotinic and Muscarinic receptors in brain
- CAN cross BBB
mechanism-
reversable inhibition of AChE -> increased local ACh (non specific) ACh everywhere
AD progression -> cholinergic neuronal loss -> diminished AChl efficacy (AChIs used to decrease AChE therefore
therapeutic uses: Alzheimer's disease
side effects- (muscarinic)
- Bradycardia
- Dizziness
- Increased urinary freq.
- GI: mausea. diarrhea (possible concern for serious GI bleed)
Non-Alzheimer's AChI's
Edrophonium
Neostigmine
Pyridostigmine (Mestinon)
Physostigmine
Ambenonium (Mytelase)
receptor selectivity- prolongs & intensifies actions of ACh on muscular nicotinic receptors in NMJ
- CANNOT cross BBB
- less effect on CNS
mechanism- reversible inhibition of AChE -> increases local ACh at NMJ on Nm receptors
Therapeutic Uses- Myasthenia Gravis Dx, NMB reversal, anticholinergic toxidrome
Side effects-
Muscarinic: salivation, urination, bradycardia, bronchoconstriction, cramping
Nicotinic: muscle cramping
GIVE EDROPHONIUM-> worsen (cholinergic) better (myasthenic)
Cholinergic Crisis: Too much ACh in NMJ
Myasthenia Crisis: Not Enough ACh in NMJ
Botulinum toxin A/B
(Botox)
receptor selectivity-local effect at muscarinic (M3) receptor (indirect parasympatholytic), nicotinic in specific locations (Wrinkles)
mechanisms- inhibits exocytosis of ACh (less receptor activation)
- Binds to VAMPs and SNAPs -> impairs vesicle fusion -> prevents ACh release
therapeutic uses- migrane, hyperhidrosis, urinary incontinence,
side effects- bruising, fatigue, soreness
Non-Depolarizing Neuromuscular Blockers (NMB's)
Pancuronium
Atracurium
Cisatracurium
Veruconium
receptor selectivity- agonsits at muscular nicotinic (Nm) receptors (sustained relaxation) LOW ACh
mechanism- muscle is unable to respond to stimulus due to impaired ability to depolarize (non-depolarizing)
therapeutic uses- Endotracheal intubation, surgery
side effects- prolonged apnea via diaphragm paralysis
Reversible with non-Alzheimers AChIs (increase ACh at NMJ to activate muscular nicotinic to reverse blockade)
Depolarizing Neuromuscular Blockers (NMBs)
Succinylcholine
receptor selectivity- depolarizing (activating) NMB at muscular nicotinic (sustained muscular contraction) MORE ACh
mechanisms- competes with ACh to MIMIC ACh and depolarize motor end plate, prolonged longer than natural ACh due to resistance to AChE
therapeutic uses- endotracheal intubation, paralysis of muscle
side effects- malignant hyperthermia (uncontrolled release of calcium from sarcoplasmic reticulum) Tx Dantrolene (muscle relaxant)
CANNOT USE non-alzheimers AChI to reverse depolarizing NMB (already too much ACh)
Belladonna (plant)
Curare (plant)
receptor selectivity- Blocks receptors
Belladonna (muscarinic receptors)
Curare (nicotinic receptors)
mechanisms- Belladonna NOT SANS not nicotinic
Curare PANS ganglia activated (nicotinic) then muscarinic may be effected
therapeutic uses: hunters use to paralyse animals, endotracheal intubation?
side effects
Cyclopentolate
Homatropine
receptor selectivity- muscarinic antagonist selective to receptors in the eyes
mechanisms-
therapeutic uses- eye drops use to dilate the pupils (mydriatic)
side effects: burning and interactions with other anticholinergics
Scopolamine
Trihexyphenidyl
Benztropine
receptor selectivity- muscarinic antagonist selective to the CNS (M1)
mechanisms- blocks muscarinic receptors (no ACh no muscle activation)
therapeutic uses- Parkinsons Disease Tx
side effects- dry mouth, constipation, urinary retnention
Ipratropium (Atrovent)
Tiotropium (Spiriva)
Aclidinium (Tudorza)
Umeclindinium (Incruse)
receptor selectivity- muscarinic antagonist RELAX bronchi (bronchiodialation)
mechanisms- blocks muscarinic receptors locally in lungs (no ACh no smooth muscle activation in lungs)
therapeutic uses- COPD; asthma
side effects-
Tolterodine (Detrol)
Fesoterodine (Toviaz)
Oxybutynin (Ditropan)
Darifenacin (Enablex)
Solifenacin (Vesicare)
Trospium (Sanctura)
Flavoxate (Urispas)
receptor selectivity- muscarinic antagonist RELAX decrease urination
mechanisms- blocks muscarinic receptors locally in bladder (no ACh no smooth muscle activation in bladder)
therapeutic uses- overactive bladder, urinary incontence
side effects
Glycopyrrolate (Robinul)
receptor selectivity- muscarinic antagonist DECREASE secretions of saliva glands
mechanisms- blocks muscarinic receptors (no ACh no secretions
therapeutic uses- peptic ulcers, severe drooling
side effects
Dicyclomine (Bentyl)
receptor selectivity- muscarinic antagonist locally in gut (decrease GI motility RELAX)
mechanisms- blocks muscarinic receptors locally in gut antispasmodic
therapeutic uses- treats symptoms of IBS
side effects
Hyoscyamine (Levsin)
receptor selectivity- central muscarinic antagonist
mechanisms- blocks muscarinic receptors
therapeutic uses- anti tremor and gut antispasmodic (IBS, colitis, kidney stones, gall stones, parkinsons
side effects
Pralidoxime (2-PAM)
receptor selectivity- muscarinic receptor antagonist
mechanism- prevents aging of covalent bond to enzyme (cholinesterase regenerator)
therapeutic uses- Tx of organophosphate toxicity
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