Cholinergic Antagonist Flashcards
Scopolamine
Isopto Hyoscine/ transderm scop. Also a tertiary I mean plant alkaloid produces Peru Friel effect similar to those of atropine although has greater action on CNS. Anti-motion sickness produces sedation but at higher doses produces excitement
Atropine
Isopto atropine. Tertiary a mean belladonna alkaloid with high affinity for muscarinic receptors. Binds competitively and prevents ACH from binding to sites. Block muscarinic activity and I resulting in mydriasis. Reduce his activity in G.I. tract low doses is a slight decrease in heart rate at higher doses causes increase in heart rate. Produces dryness of mouth
Ipatropium and tiotropium
Atrovent, spiriva handi haler. Quaternary derivatives of atropine these agents are use for bronchodilators. For treatment of bronchospasm associated with COPD. Tiotropium has the advantage of one daily dose
Tropicamide and cyclopentolate
Midryacyl/tropicacyl, ak-pentolate/cyclogyl. Ophthalmic solution for my dryasis and cycloplegia.
Benzotropine and trihexyphenidyl
Cogentin,artane. Parkinson’s disease
Darfenacin,fesoterodine,oxybutnin,solifenacin,tolterodine,trospiumchloride
Enablex,toviaz,ditropan,vesicare,detrol,sanctuary. Synthetic atropine like drugs used to treat overactive bladder blocks muscarinic receptors in bladder
Ganglionic blockers
Block nicotinic receptors of both parasympathetic and sympathetic autonomic ganglia some also block I am channels show no selectivity toward parasympathetic or sympathetic ganglia. not effective as neuromuscular antagonist
Nicotine
Depolarizes ganglia resulting in stimulation then paralysis of ganglia.
Neuromuscular blocking agents
Block cholinergic transmission between motor nerve endings and nicotinic receptors on skeletal muscle. Act as either antagonists (nondepolarizing type) Or as agonist (depolarizing type).
Neuromuscular blockers (non de polarizing competitive drugs)
Cisatracurium(nimbex), pancuronium (pavulon), rocuronium (zemuron), vecoronium.
Nondepolarizing competitive blockers drug interactions cholineesterase inhibitors
Choline esterase inhibitor’s reverse action of nondepolarizing neuromuscular blockers. However with increased dosage cholinesterase inhibitor’s can cause a depolarizing block as a result of elevated acetylcholine concentrations.
Halogenated hydrocarbon anesthetics
Drugs like desflurane enhance neuromuscular blockade by stabilizing NMJ
Aminoglycoside antibiotics
Gentamicin and tobramycin inhibit acetylcholine release from cholinergic nerves by competing with calcium ions.
Calcium channel blocker’s
Increase neuromuscular blockade of competitive blockers
Depolarizing neuromuscular blocking agents
People arrive plasma membrane of muscle fiber similar to acetylcholine. However these agents are more resistant to degradation by acetylcholine esterase. Succinylcholine is only depolarizing muscle relaxant used today.