Notes in Cholinergic and Adrenergic Pharm

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Published	02/20/2025	Q: Which sub-type of muscarinic receptor might an antagonist like (e.g. solifenacin [Vesicare]) target for the treatment of incontinence/overactive bl…
Published	02/20/2025	Q: Which sub-type of muscarinic receptor might an antagonist like (e.g. solifenacin [Vesicare]) target for the treatment of incontinence/overactive bl…
Published	02/20/2025	Q: Which sub-type of muscarinic receptor might an antagonist like (e.g. solifenacin [Vesicare]) target for the treatment of incontinence/overactive bl…
Published	02/20/2025	Other Autonomic neurotransmittersVasoactive {{c1::intestinal}} peptide (VIP)Neuropeptide Y (NPY){{c1::Calcitonin}} gene-related peptide (CGRP)ATP…
Published	02/20/2025	This is a somatic motor neuron. In this system, there’s only one neuron in the pathway from the {{c1::spinal cord}} to the {{c1::muscles}} that are in…
Published	02/20/2025	Somatic Nervous System Target tissue receptorsTarget tissue is {{c1::skeletal muscle}}Response is {{c1::contraction}}Postsynaptic receptor i…
Published	02/20/2025	Neuromuscular junction is specific to the {{c1::somatic}} nervous system Area including: presynaptic membrane of the motor neuron, the synaptic c…
Published	02/20/2025	Direct acting cholinomimetics (cholinergic agonists; parasympathomimetics)
Published	02/20/2025	Medications that enhance or activate cholinergic transmission are called {{c1::cholinomimetics}}. 1
Published	02/20/2025	Cholinomimetics can be classified as {{c1::direct-acting}} or {{c2::indirect-acting}}. 2
Published	02/20/2025	Medications that suppress or inhibit cholinergic transmission are called {{c1::cholinolytic}} or {{c2::anticholinergic}} drugs. 3
Published	02/20/2025	{{c1::Direct-acting cholinomimetics}} (cholinergic agonists) include {{c2::bethanechol, pilocarpine, and nicotine}}. 4
Published	02/20/2025	Direct-acting cholinomimetics work by mimicking {{c1::acetylcholine (ACh)}} at the receptor. 5
Published	02/20/2025	{{c1::Bethanechol}} and {{c2::pilocarpine}} are {{c3::muscarinic cholinergic receptor agonists}}. 6
Published	02/20/2025	{{c1::Nicotine}} is a {{c2::nicotinic cholinergic receptor agonist}} in the {{c3::CNS}}. 7
Published	02/20/2025	Cholinergic agonists generally have {{c1::longer-lasting effects}} than ACh but produce the same physiological response. 8
Published	02/20/2025	{{c1::Bethanechol}} is used in the treatment of {{c2::GI and urinary bladder paralysis}}. 9
Published	02/20/2025	{{c1::Pilocarpine}} is used in the treatment of {{c2::glaucoma}}. 10
Published	02/20/2025	Muscarinic cholinergic receptors are located on the {{c1::ciliary muscle}} of the eye. 11
Published	02/20/2025	Stimulation of muscarinic receptors causes {{c1::ciliary muscle contraction}}, pulling the iris back and opening {{c2::Schlemm’s canal}}, allowing flu…
Published	02/20/2025	{{c1::Nicotine}} is used to treat {{c2::cigarette withdrawal symptoms}}. 13
Published	02/20/2025	{{c1::Varenicline (Chantix)}} is a {{c2::partial nicotinic agonist}} that reduces cravings and the pleasurable effects of cigarettes. 14
Published	02/20/2025	{{c1::Bethanechol}} can cause systemic effects such as {{c2::diarrhea and incontinence}}. 15
Published	02/20/2025	Common side effects of cholinergic agonists include {{c1::bradycardia, hypotension, and bronchoconstriction}}, which may worsen asthma. 16
Published	02/20/2025	{{c1::Bethanechol}} should not be used in patients with {{c2::GI or urinary obstruction}}. 17
Published	02/20/2025
Published	02/20/2025	Indirect acting cholinomimetics
Published	02/20/2025	Cholinomimetics are also called {{c1::cholinergic agonists}} or {{c2::parasympathomimetics}} because they agonize cholinergic neurotransmission. 1
Published	02/20/2025	{{c1::Antimuscarinic drugs}} are contraindicated in patients with glaucoma because they prevent ciliary muscle contraction, causing the {{c2::iris to …
Published	02/20/2025	{{c1::Indirect-acting cholinomimetics}} inhibit acetylcholinesterase, increasing ACh in the synapse and enhancing cholinergic function. 3
Published	02/20/2025	{{c1::Neostigmine}} does not pass the blood-brain barrier (BBB), while {{c2::donepezil}} does, producing central effects. 4
Published	02/20/2025	The mechanism of action of indirect cholinomimetics is {{c1::reversible inhibition of acetylcholinesterase}}, leading to increased ACh at synapses. 5
Published	02/20/2025	{{c1::Neostigmine}} is used to treat {{c2::GI and urinary bladder paralysis, glaucoma, myasthenia gravis, and anticholinergic drug effects}}. 6
Published	02/20/2025	{{c1::Donepezil}} is used to treat symptoms of {{c2::Alzheimer’s disease}}, which is associated with the loss of cholinergic control of short-term mem…
Published	02/20/2025	Alzheimer's disease is linked to {{c1::neurodegeneration of cholinergic pathways}}, leading to loss of {{c2::short-term memory}}. 8
Published	02/20/2025	{{c1::Myasthenia gravis}} is an autoimmune disorder in which antibodies destroy {{c2::nicotinic cholinergic receptors (Nm) at the neuromuscular juncti…
Published	02/20/2025	Myasthenia gravis leads to a {{c1::70-90% reduction in nicotinic receptors}}, causing muscle weakness and rapid fatigue. 10
Published	02/20/2025	AChase inhibitors help in myasthenia gravis by {{c1::increasing ACh presence in the synapse}}, allowing more receptor activation. 11
Published	02/20/2025	Excessive cholinergic stimulation can cause {{c1::generalized parasympathetic side effects}}, with donepezil specifically causing {{c2::dizziness and …
Published	02/20/2025	AChase inhibitors are also the mechanism of action of toxins like {{c1::sarin (nerve gas) and parathion (insecticide)}}. 13
Published	02/20/2025	The antidote for AChase inhibitor poisoning is {{c1::pralidoxime (PAM)}}, which breaks chemical bonds between the toxin and AChase. 14
Published	02/20/2025	In a {{c1::myasthenic crisis}}, there is a critical lack of ACh, causing severe muscle weakness, including respiratory muscles. 15
Published	02/20/2025	In a {{c1::cholinergic crisis}}, excessive ACh overstimulates receptors, preventing muscle relaxation and causing paralysis. 16
Published	02/20/2025	Myasthenic crisis occurs {{c1::near the end of a dosing interval}} and is treated with a {{c2::cholinergic drug}}. 17
Published	02/20/2025	Cholinergic crisis occurs {{c1::soon after giving a cholinergic drug}} and is treated with a {{c2::anticholinergic drug}}, possibly requiring intubati…
Published	02/20/2025	{{c1::Sensory input}} activates memory circuits, leading to {{c2::acquisition}}, a short-term, electrophysiologic memory process. 19
Published	02/20/2025	{{c1::Repetition}} strengthens cholinergic pathways and leads to {{c2::consolidation}}, where new synaptic connections form for long-term memory. 20
Published	02/20/2025	AChase inhibitors enhance cholinergic function by {{c1::increasing ACh accumulation}}, leading to {{c2::greater receptor activation and cholinergic re…
Published	02/20/2025
Published	02/20/2025	Cholinolytic pharmacology
Published	02/20/2025	Cholinolytics are also called {{c1::antiparasympathetics}} or {{c2::anticholinergics}} because they block cholinergic neurotransmission. 1
Published	02/20/2025	{{c1::Atropine, scopolamine, and solifenacin}} are examples of cholinolytics. 2
Published	02/20/2025	Cholinolytics work as {{c1::competitive muscarinic cholinergic receptor antagonists}}, blocking ACh and reducing PNS responses. 3
Published	02/20/2025	{{c1::Atropine}} induces {{c2::mydriasis (pupil dilation)}}, reduces secretions, and treats ventricular bradycardia, severe diarrhea, and urinary inco…
Published	02/20/2025	Atropine increases heart rate by {{c1::blocking the parasympathetic (cholinergic) response}}, not by activating the sympathetic nervous system. 5
Published	02/20/2025	{{c1::Scopolamine}} is used to treat {{c2::motion sickness}} by inhibiting cholinergic activation of the emesis center. 6
Published	02/20/2025	{{c1::Solifenacin (Vesicare)}} is a selective {{c2::M3 muscarinic cholinergic receptor antagonist}} that reduces bladder muscle contraction, treating …
Published	02/20/2025	M3 cholinergic receptors are located in the {{c1::smooth muscle of the urinary bladder, GI tract, and eye}}. 8
Published	02/20/2025	M2 cholinergic receptors are located in the {{c1::heart}}, while M1 receptors are in the {{c2::salivary glands and CNS}}. 9
Published	02/20/2025	{{c1::Erythromycin}} is a CYP inhibitor that can reduce metabolism of {{c2::tolterodine (Detrol)}}, increasing its active concentration and risking an…
Published	02/20/2025	Cholinolytics suppress PNS functions, leading to side effects that are {{c1::opposite of PNS effects}}. 11
Published	02/20/2025	Cholinolytics can cause {{c1::mydriasis (pupil dilation), blurred vision, photophobia, and elevated intraocular pressure}}. 12
Published	02/20/2025	{{c1::Dry mouth (xerostomia)}} is a common reason patients stop anticholinergic medications. 13
Published	02/20/2025	Cholinolytics can cause {{c1::tachycardia and bronchodilation}} and are used in medications like {{c2::ipratropium and tiotropium}}. 14
Published	02/20/2025	In elderly patients, cholinolytics can cause {{c1::AMS (altered mental status) or hallucinations}} and block sweat glands, increasing the risk of {{c2…
Published	02/20/2025	Additional cholinolytic side effects include {{c1::urinary retention and constipation}}. 16
Published	02/20/2025	Some drugs that are not muscarinic antagonists but can produce similar blockade effects include {{c1::antihistamines, phenothiazine antipsychotics, an…
Published	02/20/2025	{{c1::Solifenacin (Vesicare) and tolterodine}} are metabolized by {{c2::CYP3A4}}, making them susceptible to interactions with CYP3A4 inhibitors and i…
Published	02/20/2025	A CYP3A4 inhibitor will {{c1::slow metabolism}} of solifenacin and tolterodine, {{c2::increasing drug levels and risk of toxicity}}. 19
Published	02/20/2025	A CYP3A4 inducer will {{c1::increase metabolism}} of solifenacin and tolterodine, {{c2::reducing drug levels and effectiveness}}. 20
Published	02/20/2025
Published	02/20/2025	Skeletal muscle relaxants/antispastic drugs
Published	02/20/2025	{{c1::Baclofen}} is a {{c2::GABA receptor agonist}} that suppresses motor neuron activity and nerve conduction. 1
Published	02/20/2025	Baclofen inhibits the release of {{c1::glutamate}}, leading to decreased {{c2::skeletal muscle contraction}}. 2
Published	02/20/2025	{{c1::Pancuronium}} is a {{c2::nicotinic receptor (Nm) antagonist}} that blocks excitation-contraction coupling, causing nondepolarizing skeletal musc…
Published	02/20/2025	{{c1::Succinylcholine}} causes {{c2::depolarizing skeletal muscle relaxation}} by activating ACh receptors but remaining bound, leading to receptor in…
Published	02/20/2025	Succinylcholine induces muscle relaxation by causing an initial {{c1::depolarization block}}, followed by a {{c2::sustained desensitization block}}. 5
Published	02/20/2025	{{c1::Botulinum neurotoxins}} inhibit {{c2::membrane fusion proteins (synaptin, SNAP-25)}}, preventing exocytosis of ACh and causing skeletal muscle p…
Published	02/20/2025	Baclofen is used to treat {{c1::spastic movement disorders}} caused by multiple sclerosis, ALS, cerebral palsy, strokes, or head injuries. 7
Published	02/20/2025	Pancuronium and succinylcholine are used for {{c1::skeletal muscle relaxation}} during surgery, tracheal intubations, and ECT therapy. 8
Published	02/20/2025	Botulinum neurotoxins are used for {{c1::strabismus, overactive bladder, chronic migraine headaches}}, and cosmetic removal of facial wrinkles. 9
Published	02/20/2025	Baclofen side effects include {{c1::CNS depression (drowsiness, dizziness, weakness, fatigue)}}, {{c2::GI symptoms (nausea, constipation), and urinary…
Published	02/20/2025	{{c1::Pancuronium and succinylcholine}} can cause {{c2::respiratory arrest and prolonged apnea}}, with decreased effects if given with a cholinesteras…
Published	02/20/2025	{{c1::Succinylcholine}} can cause {{c2::malignant hyperthermia}}, which is treated with {{c3::dantrolene}}. 12
Published	02/20/2025	{{c1::Botulinum toxin}} toxicity causes {{c2::symmetric, descending paralysis}}, requiring prolonged supportive care and {{c3::botulinum antitoxin or …
Published	02/20/2025	Neuromuscular blocking agents (NMBAs) are called {{c1::paralytics}} because they cause complete muscle flaccidity, preventing voluntary movement. 14
Published	02/20/2025	GABA neurotransmission is {{c1::inhibitory}} in the somatic nervous system and inhibits {{c2::glutamate excitatory descending pathways}}. 15
Published	02/20/2025
Published	02/20/2025	Adrenergic Pharmacology, Pharmacokinetics, general profile
Published	02/20/2025	{{c1::Catecholamines}} include epinephrine, norepinephrine, dopamine, isoproterenol, and dobutamine, and have a {{c2::benzene ring with two hydroxyl g…
Published	02/20/2025	{{c1::Noncatecholamines}} include albuterol, phenylephrine, and ephedrine and lack {{c2::hydroxyl groups}}, making them partial agonists of adrenergic…
Published	02/20/2025	Catecholamines have {{c1::low bioavailability}} when taken orally due to rapid metabolism by {{c2::intestinal and hepatic MAO and COMT}}. 3
Published	02/20/2025	Circulating catecholamines have a {{c1::short duration of action and half-life}} due to {{c2::rapid metabolism by hepatic MAO and COMT}}. 4
Published	02/20/2025	Due to the absence of hydroxyl groups, {{c1::noncatecholamines}} are {{c2::less polar/more lipid soluble}}, allowing them to pass the BBB and produce …
Published	02/20/2025	Adrenergic drugs can be administered via {{c1::eye drops, nasal mists, respiratory mists, GI, and parenteral routes}}. 6
Published	02/20/2025	The half-life of adrenergic drugs varies from {{c1::minutes (epinephrine) to hours (ephedrine)}} depending on metabolism. 7
Published	02/20/2025	Some adrenergic drugs, such as {{c1::amphetamines}}, pass the {{c2::BBB}} and cause CNS excitation. 8
Published	02/20/2025	Some adrenergic drugs exhibit high {{c1::plasma protein binding}}, such as {{c2::prazosin (97% bound)}}. 9
Published	02/20/2025	Alpha1 agonists undergo {{c1::phase I and II metabolism}}, and some oral doses (e.g., {{c2::propranolol}}) are significantly reduced by {{c3::first-pa…
Published	02/20/2025	The primary route of elimination for adrenergic drugs is {{c1::renal excretion}}. 11
Published	02/20/2025
Published	02/20/2025	Drugs that alter the biosynthesis of catecholamines
Published	02/20/2025	Drugs altering catecholamine biosynthesis include {{c1::methyl-tyrosine}} and {{c2::L-DOPA}}. 1
Published	02/20/2025	{{c1::Methyl-tyrosine}} inhibits {{c2::tyrosine hydroxylase}}, reducing all three catecholamines. 2
Published	02/20/2025	{{c1::L-DOPA}} serves as a {{c2::substrate}} for dopamine synthesis, elevating dopamine and other catecholamines. 3
Published	02/20/2025	{{c1::Methyl-tyrosine}} is used to treat {{c2::pheochromocytoma}} and severe malignant hypertension. 4
Published	02/20/2025	Pheochromocytoma can be indicated by a 24-hour urine test for {{c1::catecholamine metabolites}}. 5
Published	02/20/2025	{{c1::L-DOPA}} crosses the {{c2::BBB}} and increases dopamine in the basal ganglia, reducing parkinsonian tremors. 6
Published	02/20/2025	{{c1::L-DOPA}} is administered with {{c2::carbidopa}} to block its peripheral conversion to dopamine. 7
Published	02/20/2025	The NET is a {{c1::norepinephrine transporter}} that controls NE via {{c2::reuptake}}. 8
Published	02/20/2025	After reuptake, NE is either packaged by {{c1::VMAT}} or metabolized by {{c2::MAO}}, limiting its action. 9
Published	02/20/2025
Published	02/20/2025	Generalized sympathomimetics (not selective for any sub-type of adrenergic receptor)
Published	02/20/2025	Generalized sympathomimetics include {{c1::epinephrine}} and {{c2::dopamine}}. 1
Published	02/20/2025	Epinephrine is a nonselective adrenergic agonist acting on {{c1::alpha-1 and alpha-2}} and {{c2::beta-1 and beta-2}} receptors to induce fight/flight …
Published	02/20/2025	Dopamine is an agonist at {{c1::dopamine, D1, and beta-1}} and {{c2::alpha-1}} receptors, depending on dose. 3
Published	02/20/2025	Therapeutic uses of epinephrine include eye drops to induce {{c1::mydriasis}}, respiratory mist for {{c2::bronchodilation}} in asthma, and parenteral …
Published	02/20/2025	Dopamine treats cardiogenic shock by acting on renal D-1 receptors to increase {{c1::renal blood flow}} and on {{c2::beta-1}} receptors to boost cardi…
Published	02/20/2025	Dopamine dose effects: low dose targets {{c1::renal}} receptors, medium dose stimulates {{c1::beta-1}}, and high dose activates {{c1::alpha-1}} recept…
Published	02/20/2025	Epinephrine inhalation for asthma can cause tachycardia because it nonselectively binds to {{c1::beta-1}} receptors. 7
Published	02/20/2025	Dopamine receptors are predominantly expressed in the {{c1::kidneys}}, with additional expression in other areas. 8
Published	02/20/2025
Published	02/20/2025	Selective alpha adrenergic receptor sympathomimetics
Published	02/20/2025	{{c1::Phenylephrine}} is a selective {{c1::alpha-1 agonist}} used as a nasal decongestant and to treat priapism by causing {{c2::vasoconstriction}} in…
Published	02/20/2025	{{c1::Tetrahydrozoline}} is an {{c1::alpha-1 agonist}} that relieves eye irritation by inducing {{c2::corneal vasoconstriction}}, reducing redness fro…
Published	02/20/2025	{{c1::Clonidine}}, which crosses the BBB, is an {{c1::alpha-2 agonist}} that lowers blood pressure by reducing {{c2::catecholamine release}} and SNS t…
Published	02/20/2025	{{c1::Precedex (Dexmedetomidine HCl)}} is an IV {{c1::alpha-2 agonist}} used for sedation, contrasting with the mostly oral clonidine. 4
Published	02/20/2025
Published	02/20/2025	Selective beta adrenergic receptor sympathomimetics
Published	02/20/2025	{{c1::Isoproterenol}} is a generalized beta agonist stimulating both {{c1::beta-1}} and {{c2::beta-2}} receptors. 1
Published	02/20/2025	{{c1::Dobutamine}} is a selective {{c1::beta-1}} agonist used as a cardiac stimulant in {{c2::cardiac arrest}} and heart failure. 2
Published	02/20/2025	{{c1::Albuterol}} is a selective beta-2 agonist used as a bronchodilator, while {{c2::terbutaline}} prevents preterm birth by reducing uterine contrac…
Published	02/20/2025	{{c1::Mirabegron}} is a selective {{c1::beta-3}} agonist that relaxes the detrusor muscle, treating {{c2::urinary incontinence}} and urgency. 4
Published	02/20/2025	Selective beta agonists target receptor subtypes: {{c1::beta-1}} increases cardiac output; {{c2::beta-2}} dilates bronchi and relaxes the uterus; and …
Published	02/20/2025
Published	02/20/2025	Indirect acting and mixed acting sympathomimetics
Published	02/20/2025	Indirect and mixed sympathomimetics include {{c1::amphetamines}} and {{c2::ephedrine}}. 1
Published	02/20/2025	Amphetamines are transported into sympathetic terminals and displace {{c1::catecholamines}} to release {{c2::NE}}. 2
Published	02/20/2025	Ephedrine slowly displaces NE and acts as a weak {{c1::alpha-1}} and {{c2::beta-2}} agonist. 3
Published	02/20/2025	Amphetamines are CNS stimulants used to treat {{c1::narcolepsy}} and {{c2::ADHD}}. 4
Published	02/20/2025	Stimulants like Adderall, Dexedrine, and Ritalin enhance release of {{c1::NE}} and {{c2::dopamine}} for a calming effect in ADHD. 5
Published	02/20/2025	Concerns with amphetamine use in children include risk of {{c1::dependence}} and {{c2::drug abuse}}. 6
Published	02/20/2025	Atomoxetine (Strattera) is a selective {{c1::NE reuptake inhibitor}} for ADHD that does not release free {{c2::NE}}. 7
Published	02/20/2025	Ephedrine is used as a {{c1::nasal decongestant}} and as a {{c2::bronchodilator}}. 8
Published	02/20/2025	IV ephedrine is used in anesthesia to increase {{c1::heart rate}} and improve hemodynamics. 9
Published	02/20/2025	Ephedrine exhibits {{c1::mixed}} actions, acting both directly and indirectly as a {{c2::sympathomimetic}}. 10
Published	02/20/2025
Published	02/20/2025	Selective alpha adrenergic receptor sympatholytics
Published	02/20/2025	{{c1::Phentolamine}} is a {{c2::generalized alpha-1,2 antagonist}} that treats frostbite and Raynaud’s syndrome by reducing cutaneous vasoconstriction…
Published	02/20/2025	{{c1::Prazosin}} is a selective {{c2::alpha-1 antagonist}} that lowers blood pressure and relaxes prostatic smooth muscle to treat BPH by reducing per…
Published	02/20/2025	{{c1::Tamsulosin}} is a selective {{c2::alpha-1A antagonist}} that treats urinary obstruction in BPH by relaxing prostatic smooth muscle with minimal …
Published	02/20/2025
Published	02/20/2025	Selective beta adrenergic receptor sympatholytics
Published	02/20/2025	Examples of beta adrenergic receptor sympatholytics include {{c1::propranolol}} and {{c2::metoprolol}}. 1
Published	02/20/2025	{{c1::Propranolol}} is a generalized beta-1,2 antagonist, while {{c2::metoprolol}} is a selective beta-1 antagonist. 2
Published	02/20/2025	Both drugs treat {{c1::hypertension}}, arrhythmias, and ischemic heart disease; propranolol is also used for {{c2::migraine prophylaxis}}. 3
Published	02/20/2025	Beta-blockers lower blood pressure by blocking renal {{c1::beta-1}} receptors, reducing {{c2::renin release}}, and promoting salt/water loss. 4
Published	02/20/2025	Propranolol’s nonselective blockade can cause {{c1::bronchoconstriction}}, unlike the more selective {{c2::metoprolol}}. 5
Published	02/20/2025	Beta-blockers reduce cardiac output, activating {{c1::carotid baroreceptors}} and triggering a compensatory {{c2::vasomotor response}}. 6
Published	02/20/2025
Published	02/20/2025	Combined alpha and beta-AR sympatholytic
Published	02/20/2025	Labetalol is a combined {{c1::alpha}} and {{c2::beta}} AR antagonist. 1
Published	02/20/2025	Labetalol lowers blood pressure by reducing cardiac output via {{c1::beta-1}} blockade and blocking compensatory vasomotor response via {{c2::alpha-1}…
Published	02/20/2025
Published	02/20/2025	Pharmacotoxicology of adrenergic drugs
Published	02/20/2025	Sympathomimetics cause side effects such as {{c1::CNS agitation}} and {{c2::tremors}}, along with insomnia, HTN, tachycardia, dysrhythmias, angina, hy…
Published	02/20/2025	Sympatholytics produce adverse effects including {{c1::orthostatic hypotension}} and {{c2::fatigue}}, plus exercise intolerance, bronchoconstriction, …
Published	02/20/2025	Amphetamine is a {{c1::Schedule II}} drug that rapidly develops {{c2::tolerance}}. 3
Published	02/20/2025	Antagonistic interactions occur when {{c1::ephedrine}} is combined with {{c2::propranolol}}, opposing each other’s effects. 4
Published	02/20/2025	Addictive interactions are observed with the combination of {{c1::prazosin}} and {{c2::propranolol}}, potentially increasing dependency risks. 5
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