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114 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Pirenzepine
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M1 competitive antagonist
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No clinical use yet
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Muscarine
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Muscarinic receptor agonist
Mimics effects of Ach M1-M5 GPCR receptor |
CV and Smooth muscle and glands
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Nicotine
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Nicotinic receptor agonist
Mimics effects of Ach Ng and Nm ligand gated receptor |
Ganglia and NMJ
Depolarization blockade |
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Arecoline
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Betel nut
Cholinomimetic alkaloid Chewed for intoxicating effect |
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Pilocarpine
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Stimulates muscarinic receptors
Tx of open angle glaucoma by opening Canals of Schlemm (also with Brimonidine) Tx of xerostomia |
Relief of dry mouth (hypofunction of salivary glands) Sjogrens syndrome, cancer radiotherapy
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Salagen
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Tx of xerostomia
Pilocarpine like Muscarinic agonist |
Relief of dry mouth due to hypofunction of salivary glands - Sjogrens syndrome, cancer radiotherapy
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Bethanechol
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Cholinomimetic
GI stimulation Tx of urinary retention |
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Carbachol
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Cholinergic agonist
Ocular (Surgery or Glaucoma) Constrict pupils during cataract surgery |
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Methacholine
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Cholinomimetic
Provocative test for hyperreactive airways |
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Bethanechol
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Cholinomimetic
GI stimulation Tx of urinary retention |
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Carbachol
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Cholinomimetic
Ocular (Surgery or Glaucoma) |
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Methacholine
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Cholinomimetic
Provocative test for hyperreactive airways |
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Atropine
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Muscarinic receptor antagonist
Pupillary dilation |
Atropa belladonna (Mona Lisa)
Jimson weed inhale to treat asthma |
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Glycopyrrolate
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Antimuscarinic (muscarinic receptor antagonist)
Preanesthetic to reduce secretions |
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Scopolamine
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Antimuscarinic that is highly lipophilic = selectivity for CNS
Tx of motion sickness |
SE= dry mouth, blurred vision, sedation, confusion and psychosis at high doses
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Meclizine
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anti-histamine (H1 receptor blocker)
Antivert Tx of vertigo and motion sickness |
SE = anti-muscarinic effects similar to atropine such as dry mouth, blurred vision, constipation, urinary retention
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Ipratropium
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Antimuscarinic similar to atropine
Tx of asthma and COPD Atropine is lipid soluble and can cause CNS and other SE. Ipratropium has a quat. nitrogen group = low CNS and other SE |
Atrovent
Quaternary nitrogen = poor absorption Toxic doses cause nicotinic toxicity like effects: hypotension (ganglionic blockade) and muscular weakness (NMJ blockade) |
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Combivent
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Ipatropium + albuterol
Antimuscarinic + beta2 agonist |
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Spiriva (Tiotropium)
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long acting analog of combivent (ipatropium + albuterol) = antimuscarinic + beta2 agonist
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Tolterodine
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Detrol
Antimuscarinic nonselective (M1-M5) Tx of overactive bladder Reduces urinary retention |
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Solifenacin
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Vesicare
M3 selective muscarinic receptor antagonist |
Lower incidence of constipation
Lower incidence of confusion |
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Darifenacin
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Enablex
M3 selective muscarinic receptor antagonist |
Lower incidence of constipation
Lower incidence of confusion |
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Propantheline
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Antimuscarinic (muscarinic receptor antagonist)
Preanesthetic to dry secretions |
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Nicotine
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Nicotinic receptor agonist
Tx of smoking cessation |
Cholinergic effects at all autonomic ganglia including adrenal medulla, NMJ, CNS
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Varenicline
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Chantix
neuronal nicotinic receptor partial agonist in CNS Tx of smoking cessation SE = Nausea (30%) |
Produces low-moderate release of dopamine at reward centers in brain, mimick nicotine's effect = reduce withdrawal symptoms
Blocks binding of nicotine and the + reinforcement obtained through smoking |
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Hexamethonium
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ganglionic nicotinic receptor antagonist
Causes paralysis of entire autonomic system |
Tx of HT, dissecting aortic aneurysm, autonomic hyperreflexia, hemorrhage in surgery
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Mecamylamine
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Trade name: Inversine
Ganglionic nicotinic receptor antagonist Causes paralysis of entire autonomic system |
Tx of HT, dissecting aortic aneurysm, autonomic hyperreflexia, hemorrhage in surgery
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Edrophonium
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Competitive cholinesterase inhibitor
Tensilon test - diagnostic Occlude active site (occupies aligning site, Ach can't bind) |
Reversible AchE inhibition b/c competitive blockade
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Tacrine
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Competitive cholinesterase inhibitor
Cognex Treatment of Alzheimers |
Reversible AchE inhibition b/c competitive blockade
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Donepezil
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Competitive cholinesterase inhibitor
Aricept |
Reversible AchE inhibition b/c competitive blockade
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Physostigmine
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Carbamylated:AchE
Reversible |
Mechanism: serves as substrate and forms more stable (but still reversible) enzyme-substrate complex
ESERINE (witch trials) Substrate inhibitor of Ach Binds to site of Ach nucleophilic attack with better affinity than Ach |
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Neostigmine
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Carbamylated:AchE
Reversible |
Mechanism: serves as substrate and forms more stable (but still reversible) enzyme-substrate complex
Binds to site of Ach nucleophilic attac with better affinity than Ach Forms carbamylated enzyme + choline |
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Pralidoxime (2-PAM)
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Antidote for acute organophosphate intoxication
Oxime - Tx quickly due to aging! |
Have higher affinity for organophosphate - attack organophosphate and pulls off of enzyme
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Therapeutic use for neostigmine
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1. Paralytic ileus
2. Bladder atony 3. Alzheimer's disease 4. Myasthenia gravis |
Reversible AchE inhibitor
Carbamylated:AchE (slow hydrolysis to regenerate enzyme = Increased Ach) |
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Therapeutic use for echothiophate
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Glaucoma
Organophosphate Irreversible AchE inhibitor Parasympathomimetic |
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Therapeutic use for tacrine or donezepil
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Alzheimers Disease
Parasympathomimetic and centrally acting AchE inhibitor Marketed as Cognex |
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DUMBELS
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Diarrhea
Urination Miosis Bronchospasm/Bradycardia Emesis (vomiting) Lacrimation Salivation |
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Echothiophate
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Organophosphate
Irreversible |
Forms stable enzyme-substrate complex by phosphorylation
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Sarin
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Military nerve gas
Organophosphate Irreversible |
Forms stable enzyme-substrate complex by phosphorylation
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VX
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Military nerve gas
Organophosphate Irreversible |
Designed to be absorbed through any part of anatomy
Forms stable enzyme-substrate complex by phosphorylation |
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Malathion
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Organophosphate
Insecticide Selectivity in insects only |
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Parathion
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Organophosphate
Insecticide Toxic to humans; no selectivity to insects or humans |
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Tx of Sarin/VX organophosphate intoxication
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2-PAM + Atropine (N + M effects)
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Sympathetic innervation of sweat gland is _____
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Cholinergic
Ach |
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Postganglionic neurotransmitter at adrenal medulla
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Epinephrine
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Postganglionic neurotransmitter at sweat glands
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Ach
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Post ganglionic neurotransmitter at renal vasodilator fibers
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Dopamine
Causes vasodilation |
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Enzyme catalyzing Tyrosine --> Dopa
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Tyrosine hydroxylase
Occurs in the cytoplasm |
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Metyrosine
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Competitive inhibitor of tyrosine hydroxylase
Depletes catecholamines everywhere Tx of Pheochromocytoma |
SE: Weight gain b/c of reduced metabolism secondary to NE and E depletion
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False transmitter
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Alpha methyl norepinephrine
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Enzyme catalyzing Tyramine --> Octopamine
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Dopamine beta hydroxylase
This enzyme is promiscuous Produces false transmitter Decrease in sympathetic nervous activity - does NOT work at synapse |
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Guanethidine
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Inhibition of the Na+ATPase dependent pump
Blocks sympathetic nerve terminals Blocks initial NE release Sympathetic neuron blocker |
Reduces release of catecholamines
Inhibition of Na+/K+ ATPase pump HT treatment |
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Reserpine
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Blocks adrenergic neurons
VMAT = vesicular monoamine transporter Blocks uptake into the storage vesicles! Depletes stored NE Tx of HT, but severe depression Never give to depressed patients, will cause severe depression |
HT control via peripheral and central mechanism
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Cocaine
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Monoamine reuptake inhibitor (uptake I)
Increase blood pressure and heart rate CNS: euphoria, increased alertness, arousal |
Local anesthetic
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Imipramine
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Tricyclic antidepressant
Inhibitor of monoamine reuptake |
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Sites containing MAO
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Monoamine nerve terminals
Liver, Kidney, Gut (mucosa and flora) High concentration in mitochondria |
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Site with highest activity of COMT
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Liver
Catechol-O-methyl transferase |
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Entacapone
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COMT inhibitor
Tx adjunct therapy of Parkinsons |
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MAO-I
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Monoamine oxidase inhibitor
Antidepressant |
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Wine-and-Cheese syndrome
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Wine + cheese + MAO-I = Hypertensive crisis
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Tyramine (DBH) --> Octopamine which is a false transmitter (inactive at adrenergic receptors)
Tyramine itself = indirect sympathomimetic activity Elicit hypertensive crisis - death due to stroke/CVA |
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Norepinephrine
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Acts at alpha and beta1 receptors
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Isoproterenol
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Acts at beta1 and beta2 receptors
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Epinephrine
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Acts at alpha, beta1, and beta2 receptors
Tx of acute anaphylaxis/cardiac arrest Adjunct with local anesthetics |
Epinephrine + Xylocaine
E given to vasoconstrict the blood vessels and keep anesthetic localized longer |
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EPI Reversal
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Give phentolamine (nonselective alpha antagonist)
Leaves action of E with only beta1 and beta2. Beta2 = vasodilation = decreased blood pressure |
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Alpha1 receptor function (List 5)
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Vasoconstriction (innervated)
Pupillary dilation Ejaculation Inhibit micturition GI inhibition |
E>NE>>I
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Alpha2 receptor function
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Vasoconstriction (uninnervated)
Prejunctional inhibition of NE release |
NE>E>>I
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List effects of NE on pulse rate (HR), blood pressure, and peripheral resistance
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Pulse rate (HR): decrease
Blood pressure: increase Peripheral resistance: increase |
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List effects of E on pulse rate (HR), blood pressure, and peripheral resistance
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Pulse rate (HR): no change (b/c no change in MABP)
Blood pressure: increase systolic (alpha), decrease systolic (beta2), no change MABP Peripheral resistance: no change |
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List effects of I on pulse rate (HR), blood pressure, and peripheral resistance
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Pulse rate (HR): increase (slight)
Blood pressure: decrease (beta2) Peripheral resistance: decrease |
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Beta1 receptor function
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Cardiac stimulation (innervated)
Renin secretion |
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Beta2 receptor function
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Cardiac stimulation (uninnervated)
Bronchodilation Uterine relaxation GI inhibition Vasodilation (uninnervated) |
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Primatene mist
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Bronchodilator
Very low dose |
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Epinephrine with xylocaine
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Adjunct with local anesthetic
Vasoconstriction (alpha1 receptor) to keep the anesthetic in area longer |
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Epipen
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Epinephrine tx against anaphylaxis
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Phenylephrine
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Alpha1 agonist
In nasal decongestants Tx of Paroxysmal atrial tachycardia (PAT) |
Pacemaker causing tachycardia very responsive to vagal stimulation. To turn on vagus, must increase BP and trigger baroreceptor reflex. Patient returns to sinus rhythm.
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Ephedrine/Pseudoephedrine
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Indirect sympathomimetic
Nasal decongestants (Sudafed) Vasoconstriction of blood vessels to relieve swelling in nasal mucosa. CNS effects: stimulant - amphetamine like action Has some direct adrenergic action |
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MAO-Inhibitor and indirect sympathomimetic interaction
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Potentiation!
Dangerous increase in BP |
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Amphetamine (Adderall)
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Mixed action adrenergic agent (alpha and beta agonist)
Appetite suppressant Tx of ADHD and narcolepsy CNS active = tolerance, abuse, cardiac arrhythmia, increased BP and stroke |
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Methamphetamine
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Appetite suppressant
CNS active = tolerance, abuse, cardiac arrythmia, increased BP and stroke |
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Methylphenidate
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Ritalin
Amphetamine like CNS stimulant Mixed adrenergic alpha and beta agonist Tx of ADHD |
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Imidazoline
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Alpha receptor agonist used locally for nasal decongestant and in eyedrops
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Naphazoline
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Visine
alpha agonist Vasoconstriction "get the red out" |
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Oxymetazoline
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Visine
alpha agonist Vasoconstriction "get the red out" |
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Clonidine
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Catapres
alpha2 agonist We thought it caused prejunctional inhibition of NE release (negative feedback) REALLY: Acts CNS brainstem to decrease sympathetic nervous system activity Tx of HT |
SE: dry mouth, withdrawal syndrome
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Albuterol
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Beta2 selective agonist
Bronchodilation Tx of asthma (acute rescue tx) Eg: Proventil, Ventolin |
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Formoterol
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Long-acting (12 hours) slow onset bronchodilation
Beta2 selective agonist Tx of asthma |
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Salmeterol
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Long-acting (12 hours) slow onset bronchodilation
Beta2 selective agonist Tx of asthma |
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Ritodrine
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Beta agonist
Prevent premature labor Uterine relaxation Give PO or IV SE: Tachycardia |
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Dobutamine
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Beta1 receptor agonist
(but also acts at alpha and beta2) Cardiac stimulant Inotropic > chronotropic |
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Dopamine
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D1 receptor agonist
Vasodilation in kidney Also have indirect sympathomimetic activity at alpha and beta receptors Can cause SHOCK |
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Phentolamine
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Nonselective competitive alpha blocker
EPI reversal phenomenon 1. Blocks NE receptor 2. Blocks prejunctional alpha2 receptor With baroreflex, nerver terminal releases more NE = binds to beta1 and causes greater cardiac stimulation |
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Phenoxybenzamine
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Non-competitive irreversible alpha blocker
Give with phenylephrine tx of Pheochromocytoma |
Given with phenylephrine (alpha agonist) will look competitive at first, then look noncompetitive.
SPARE RECEPTORS |
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Prazosin
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Alpha1 selective competitive antagonist
Tx of HT, CHF, BPH Minipress "First dose phenomenon" |
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Terazosin
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Alpha1 selective competitive antagonist
Tx of HT, CHF, BPH Hytrin "First dose phenomenon" |
Tell patient to take before bed so orthostatic hypotension can be avoided
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Doxazosin
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Alpha1 selective competitive antagonist
Tx of HT, CHF, BPH Cardura "First dose phenomenon" |
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Tamsulosin
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Flomax
Alpha1 selective antagonist Selective effect on urinary flow Tx of BPH w/ lower incidence of orthostatic hypotension |
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Indications for Beta Blockers (5)
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1. Angina
2. Cardiac arrhythmia 3. Hypertension 4. Post-myocardial infarction 5. Congestive heart failure |
Beta blockers do not lower blood pressure in normotensive individuals
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Propanolol
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Inderal
Competitive antagonist at beta receptor Nonselective "First pass effect" |
ADR: Cardiac depression, bronchoconstriction, hypoglycemia, CNS effects (sedation, nightmares, insomnia)
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Metoprolol
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Beta1 selective antagonist
Lopressor/Toprol Tx of HT, angina, cardiac arrhythmia, ischemic heart disease, CHF |
Problem: T1/2 = 3-4 hours
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Atenolol
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Tenormin
Beta1 selective antagonist Renal elimination QD dosing (T1/2 = 6-9 hrs) |
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Pindolol
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Visken
Partial agonist at all beta receptors Indirect sympathomimetic activity This means that apart from blocking beta-adrenoceptors it produces some stimulation. Pindolol therefore only slightly influences normal sympathetic drive at rest but effectively reduces the effects of elevated sympathetic activity. |
Less cardiac depression
Less bronchoconstriction Reduce peripheral resistance |
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Esmolol
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Ultra short acting beta blocker
Inhibition of tachycardia Susceptible to enzymatic hydrolysis in blood IV use in Surgery |
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Carvedilol
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Third generation beta blocker
Antioxidant activity Tx of angina, HT, ischemic heart disease, CHF, cardiac arrhythmia |
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Tyramine
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Indirect sympathomimetic
Gets in by uptake pump so blocked by Cocaine |
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Tachyphylaxis
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Special case of tolerance that happens very quickly
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Pyridostigmine
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Give to troops with potential exposure to VX
Protecting some of their Cholinesterase (Carbamylated) will regenerate spontaneously Phosphorylated ChE will not. |
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-Oxime
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Pralidoxime (2-PAM)
Antidote for acute organophosphate intoxication Tx quickly b/c of "aging" |
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"Aging"
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Oximes have a large alkyl group that is necessary but unstable. Aging is when the alkyl group falls off, becomes stable, and also nonfunctional.
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Tensilon Test
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Test to help dx Myasthenia Gravis
Edrophonium given IV. Patient is asked to peform repetitive muscle movements. Observe to see if muscle strength is improved by Tensilon. |
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Nicotine gum/patch
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Smoking cessation
Low side effects of nicotine because it is low dose |
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Brimonidine
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alpha2 agonist
Tx of glaucoma Reduce intraocular secretions to decrease intraocular pressure |
Another way to tx glaucoma:
Pilocarpine: muscarinic agonist = open up Canals of Schlemm to increase drainage of aqueous humor |
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Fast Mushroom Poisoning
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Fly agaric (Amanita muscaria)
Symptoms on card 3 |
*Bradycardia
*Nausea, cramps, vomiting, diarrhea *Bronchoconstriction *Salivation *Sweating *Visual disturbances *Hypotension |
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Uninnervated muscarinic receptors mediate vasodilation via ___
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NO
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Botulinum toxin (botox)
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Enters cholinergic nerve terminals and destroys synaptic proteins involved in exocytic release of Ach.
Used clinically to reduce wrinkles. (Relaxation of muscles by working at the preNMJ receptors) |
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