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Pharm
autonomic nervous system
Question | Answer |
---|---|
Efferent Neurons | leaving the CNS; pre & post-ganglionic neurons; divided into sympathetic and parasympathetic nervous systems |
Sympathetic pathway of acetylcholine transmission | Ach -->nicotinie receptor -->adrenergic postganglionic neurons -->norepi-->adrenergic receptor (alpha or beta) |
Parasympathetic pathway | pre is longer than post; Ach-->nicotinic-->cholinergic postganglionic neuron-->Ach-->cholinergic receptor (muscarinic @ tissue levvel) |
Acetylcholine | 1.synthesis of Ach 2. Uptake into storage vesicles 3. release of neurotransmitter (blocked by botulinum toxin) 4. binding to receptor activates postsynaptic receptor 5. degradation of ach by acetylcholinesterase in synaptic cleft 6. recycling of choline |
Norepinephrine | 1. synthesis-hydrolization of tyrosine 2. uptake into vesicles-dopamine converted to NE 3. release of neurotransmitter-Ca helps bind to membrane 4. binding to receptor 5. removal of NE-reuptake or 6. metabolism-methylated by COMT and oxidized by MAO. |
Muscarinic Receptors | ganglia of parasympathetic nervous system, autonomic effector organs; slower response b/c involves G proteins, causes breakdown of M1 & M3 |
Nicotinie Receptors | autonomic ganglia, neuromuscular junction; IP3 opens calcium channels in endoplasmic reticulum |
SE of direct acting cholinergic drugs | diarrhea, diaphoresis, miosis, nausea, urinary urgency |
Anticholinesterases (AChEs) | *reversible-used at junction for myasthenia gravis (skeletal muscle autoimmune disease), tx for OD c Ach drugs & for Alzheimers disease-tacrine increases Ach levels; *Irreversible-developed by military as nerve agents |
Physostigmine | reversible AchE; to tx glaucoma to reduce intraocular pressure; adverse effects include contraction of visceral smooth muscle, miosis, hypotension, bradycardia |
Bethanechol | prototype of direct acting cholinergic, used post-op to stimulate GI tract & to tx urinary retention |
Antimuscarinic agents | -used to tx Parkinson's disease, asthma, & arrythmias; *ATROPINE-bind to muscarinic receptors competitively to inhibit Ach |
Anticholinergic effects | Opposite of PNS functions; *blurred vision *confusion *mydriasis *constipation *urinary retention |
Ganglionic blockers | not used often; high incidence of SE limit use; NICOTINE & TRIMETHAPHAN-used as hypotensive agent during surgery |
Neuromuscular junction transmission inhibitors | Nondepolarizing-TUBOCURARINE-doesn't allow ion channel to open; Depolarizing-SUCCINYLCHOLINE-sensitizes receptor |
Alpha1 receptors | vasoconstriction, doesn't affect lungs |
Alpha2 receptors | inhibits NE release, works presynaptically to regulate release of ligand that binds to NE; also inhibits insulin release |
Beta1 receptors | tachycardia, increased myocardia contractility, increases renin's release |
Beta2 receptors | vasodilation in muscles; bronchodilation, increased release of glucagon |
Alpha receptors in general | found mainly on smooth muscle; used to increase BP, as decongestant (OXYMETAZOLINE), and in ophthamology to dilate pupils; A1 receptors-activation increases DAG and IP3 production leaving to increase ca ions in cell |
Beta receptors in general | found on both cardiac and smooth muscle membranes; B1-in heart, increased rate and force of contraction, B2-smooth muscle-vasodilation of skeletal & bronchodilation |
PHENYLEPHRINE | non selective alpha1 agonist for nasal decongestion, to raise blood pressure, and to tx tachycardia |
ALBUTEROL | B2 direct acting agonist; short acting tx of bronchospasm |
CLONIDINE | a2 direct acting agonist; tx hypertension |
DOBUTAMINE | B2 direct acting agonist; tx congestive heart failure |
EPINEPHRINE | direct acting agonist on all receptors; to tx acute asthma, open-angle glaucoma; anaphylactic shock, local anesthetic to increase duration of action |
EPHEDRINE | direct and indirect action; to tx asthma, nasal decongestant, to raise BP |
Side effects of adregergic agonists | *arrhythmias *headache * hyperactivity *insomnia *nausea *tremors |
PRAZOSIN | alpha1 blocker to tx htn & heart failure |
beta blockers | to tx CVD-slow rate and lower BP; to tx angina, htn, arrhythmias |
Alpha2 agonists | Clonidine; to tx htn-decrease sympathetic output presynaptically; for migraine prophylaxis-decreased vascular tone |
ATENOLOL | B1 blocker |
PROPRANOLOL | non specific beta blocker to tx htn, glaucoma, migraine, hyperthyroidism, angina, MI |
COCAINE | adrenergic antagonists; affects neurotransmitter uptake or release |