PNS pharmacology Flashcards
Drug inhibiting step 2 (storage): Ach stored in VAT
Vesamicol
Rate-limiting step in Cholinergic pathway
Conversion of Acetyl-Coa and Choline to Ach by ChAT
Drug altering synaptobrevins (SNARE proteins triggered by Ca) to prevent release of ACh (Step 3)
Botulinum toxins
3 drugs inhibiting degradation of Ach to choline & acetate by acetylcholinesterase (Step 4/ termination)
Carbamates
Organophosphates
Neostigmine
Types of NS that causes erection and ejaculation
Erection: PNS; Ejaculation: SNS
Point & Shoot
Parasympathetic NS have _______ PREganglionic fibers & ______ POSTganglionic fibers.
Long; Short
PLaSma
Gq-coupled cholinergic receptor (inc in IP3 & DAG) in nerve endings
M1
Gi-coupled cholinoreceptor found in heart and some nerve endings (dec cAMP)
M2
Gq-coupled cholinoreceptor which relaxes bronchial smooth muscles and increase GI secretion
M3
Blocks step 1 (synthesis) of Ach from acetyl-CoA + choline
Hemicholinium
Direct-acting cholinomimetic (M1-3) used for bladder and bowel atony post-op
Betanechol
Direct-acting cholinomimetic (M3 in ciliary m & salivary g) used in glaucoma, sjogren & sicca syndrome
Pilocarpine
Autoimmune disorder characterized by xerostomia, xerophthalmia, rheumatoid arthritis
Sjogren syndrome
Direct-acting cholinomimetic (Nn, Nm) used for smoking cessation
Nicotine
Indirect-acting cholinomimetic MOA
Binds to cholinesterase
Indirect-acting cholinomimetic used in tensilon test for myasthenia gravis; very short-acting (5-15 mins)
Endrophonium
Indirect-acting cholinomimetic with muscarinic effects blocked by atropine & pralidoxime
Neostigmine
Autoimmune destruction of nicotinic Ach receptors characterized by fluctuating muscle weakness and ocular symptoms (ptosis, lagophthalmos)
Myasthenia gravis
Acute worsening of MG symptoms due to infx, stress or undermedication
Myasthenic crisis
Excessive activation of cholinoreceptors due to overmedication (skeletal m weakness and ParaSy signs)
Cholinergic crisis
Endrophonium ______ muscle strength in cholinergic crisis.
weakens
improves in myasthenic crisis
Indirect-acting cholinomimetic used for Alzheimer’s disease
Rivastigmine
Donepezil
Galantamine
What type of poisoning presents with the ff sx:
Diarrhea, urination, miosis, bronchospasm, bradycardia, excitation (CNs, skeletal m), lacrimation, sweating, salivation
Organophosphate poisoning
DUMBBELSS
Cholinergic antagonist blocking all M receptors, 1st choice in organophosphate poisoning; used as mydriatic and cyclopegic
Atropine
Cholinesterase regenerator; binds phosphorus of organophosphate; used in nerve gas poisoning
Pralidoxime
Cholinergic antagonist (all M) reducing tremors more than rigidity in Parkinson’s
Benztropine