Term
| Direct acting Cholinergic agonists |
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Definition
Bethanechol (Urecholine)
Pilocarpine (Isopto Carpine, Pilocar)
Cevimeline (Evoxac)
Nicotine
Varenicline (Chantix) |
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Term
Cholinesterase Inhibitors
"Indirect acting"
increase ACh @ M and N receptors |
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Definition
Edrophonium (Tensilon)
Neostigmine (prostigmin)
Physostigmine (Eserine)
Echothiophate
Doneprezil (Aricept)
Organophosphates
Pralidoxime (2-PAM) |
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Term
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Definition
Atropine
Scopolamine (transderm scop)
Glycopyrrolate (Robunil)
Dicylomine (Bentyl)
Tolterodine (Detrol)
Oxybutynin (Ditropan)
Darifenacine (Enablex)
Ipratropium (Atrovent)
Tropicamide (Mydriacil)
Benzotropine (congentin) |
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Term
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Definition
Direct-acting cholinergic agonist
-selective for M receptors
-activates G-protein-IP3-DAG-ca-proteinK
-does not cross BB barier
-effects seen most in Urinary & GI ( most commonly used to stimulate peristalsis)
-M2 binding=inhibitory (dec adenylyl cyclase) |
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Term
| Pilocarpine (Isopto Carpine, Pilocar) |
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Definition
Direct-acting cholinergic agonist
-Most common Cholinergic Glaucoma treatment (closed-w/ cholinesterase inhibitor & open)
-specific for M receptors
-activates G-protein-IP3-DAG-Ca-proteinK
-well absorbed
-gets into brain easily
-big effect on Sweat & salivary glands-profuse seating w/ M1 receptors
-M2=inhibitory (dec adenylyl cyclase) |
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Term
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Definition
direct-acting cholinergic agonist
-selective for M3 receptors
-activates G-protein-IP3-DAG-Ca-proteinKin
-M2=inhibitory (dec adenylyl cyclase)
-Commonly used to increase salivation in treatment of Sjogren's syndrome |
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Term
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Definition
direct acting cholinergic agonist
-selective for N receptors
-help people quit smoking
-due to autonomic ganglion stim-get firing of PNS & SNS
-cardiac: maily sympathetic
-GI: mainly parasympathetic |
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Term
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Definition
direct acting cholinergic agonist
-partial agonist on brain N receptors
-help people quit smoking: low levels of DA, blocks effects of nicotine if smokes
-Side effects: nausea, vomiting, GI, sleep disturbance, nightmares, psychosis |
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Term
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Definition
cholinesterase inhibitor
-must be injected
-binds reversibly, short duration of action (5-10min)
-quaternary ammonium compound
-diagnosis of myasthenia gravis!
-reversal of neuromuscular blockade in surgery |
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Term
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Definition
cholinesterase inhibitor
-covalent bond (30min-6hrs)
-quaternary amine, not well absorbed orally
-treat chronic Myasthenia gravis! (orally)
-doesn't cross BB barrier
-OLD drug for paralytic ileus/atony of bladder-not used anymore
-reversal of neuromuscular blockade in surgery |
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Term
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Definition
cholinesterase inhibitor
-covalent bond (30min-6hrs)
-tertiary amine, absorbed orally
-will get into Brain bad CNS effects, so NOT used orally
-directly in eye to treat open angle glaucoma! |
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Term
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Definition
cholinesterase inhibitor
-is an organophosphate
-long duration of action
-long term control of intraocular pressure (can be used for open angle glaucoma) |
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Term
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Definition
cholinesterase inhibitor
-absorbed orally, get into brain
-treat Alzheimer's disease |
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Term
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Definition
cholinesterase inhibitor
-highly lipid soluble
-long lasting bond. "AGING"-becomes irreversible.
-2PAM can prevent aging if added soon enough
-if aging not prevented-poisoning can be fatal! |
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Term
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Definition
cholinesterase inhibitor
-given to treat Organophosphate poisoning (prevent aging) |
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Term
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Definition
cholinergic antagonist
-treat Organophosphate/carbamate poisoning (irreversible cholinesterase inhibitors)
-does not enter CNS well until high doses
-salivary, sweat glands, bronchial tissues affected at low doses
-ANS, Heart, GI-high doses
-reverse effects of reflex vagal discharge
-reverse bradycardia produced by M agonists or cholinesterase inhibitors
-in MI to decrease bradycardia or AV block |
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Term
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Definition
cholinergic antagonist
-enters CNS easily (can get toxic psychosis)
-sedation, amnesia
-absorbed through skin as well
-treat/prevent motion sickness
-pre-anesthetic regimen. sedation, amnesia, dry secretions |
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Term
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Definition
cholinergic antagonist
-prevent vagal response during surgery
-decrease muscharinic side effects w/ myasthenia gravis treatments |
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Term
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Definition
cholinergic antagonist
-inhibits motility and secretions in GI track
-antispasmodic |
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Term
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Definition
cholinergic antagonist
-M3 antagonist
-treat overactive bladder, bladder spasms
-not lipid soluble, few CNS side effects
-Preferred drug of elderly |
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Term
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Definition
cholinergic antagonist
-prevent bladder spasm after prostate surgery |
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Term
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Definition
cholinergic antagonist
-competitive, M3 antagonist
-treat overactive bladder
-taken orally, has many drug metabolism interations (CYP2D6 & CYP3A4) |
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Term
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Definition
cholinergic antagonist
-quaternary ammonium compound
-not well absorbed, effects limited to lung
-bronchodilation (COPD) |
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Term
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Definition
cholinergic antagonist
-short-acting mydriasis & cycloplegia (eye exams) |
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Term
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Definition
cholinergic antagonist
-used to restore balance between Ach & DA (antipsychotic drugs, parkinson's disease)
-decrease extrapyramidal symptoms |
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Term
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Definition
Epinephrine (Adrenalin)
Norephinephrine (Levophed)
Isoproterenol (Isuprel) |
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Term
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Definition
Phenylephrine (Neo-synephrine)
Pseudoephedrine (Sudafed)
Oxymetazoline (Afrin) |
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Term
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Definition
Clonidine (catapres)
Apraclonidine (Iopidine) |
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Term
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Definition
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Term
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Definition
Albuterol (Ventolin)
Ritrodine (Yutopar) |
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Term
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Definition
Dopamine (Intropin)
Fenodolpam (corlopam) |
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Term
| "other" adrenergic stimulants |
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Definition
Ephedrine
Amphetamine
Cocaine
Tyramine |
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Term
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Definition
Catecholamine
-affect alpha1 (excitatory-IP3-DAG-PKC) & alpha2 (inhibitory-inhibit adenylyl cyclase-dec cAMP) receptors
-High affinity for B2 receptors
-effect depends on dose administered
-overall: increase in PP, little change in overall pressure, Inc HR
-Inc Rein secretion (B1)
-Bronchodilation (B2)-emergency asthma treatment
-treat anaphylactic shock
-emergency treatment of cardiac arrest, and complete heart block
-treat glaucoma, inc removal and dec production of aqueous humor
-decrease diffusion of local anesthetics |
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Term
| Norepinephrine (Levophed) |
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Definition
Catecholamine
-affect alpha1 & alpha2 & B1 receptors
-little effect on B2 receptors!
-more effect on B3 receptors
-must be injected, rapid metabolism
-vasoconstriction-inc TPR-inc BP
-DBP & SBP increase, little change to PP
-if atopine given before-vagal reflex inhibited-HR will increase
-NE can cause severe vasoconstriction & then necrosis at infusion site |
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Term
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Definition
Catecholamine
-potent selectie B1 & B2 agonist
-does not work on alpha receptors
-used in emergency treatment for cardiac arrest and complete heart block
-sort increase in BP, overall DEC in BP
*lg doses can cause tachycardia, palpitations, arrhythmias
-high affinity for all B receptors |
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Term
| Phenylephrine (Neo-synephrine) |
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Definition
Alpha agonist
-alpha 1 selective
-vasoconstriction-increases TPR-INC BP-reflex dec HR
-used in hypotensive emergency to raise BP
-careful w/ hypertensive pts
-mydriasis w/o affecting accommodation for eye exams |
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Term
| Pseudoephedrine (Sudafed) |
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Definition
Alpha agonist
-OTC decongestant prep
-use w/ caution w/ hypertension (may inc BP)
-can be used to make Meth |
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Term
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Definition
Alpha agonist
-used topically as nasal sprays as decongestants
-rebound effects (down regulated receptors)
-also works on alpha-2 receptors-can cause hypotension in lg quantity
**contraindicated in narrow-angle glaucoma & Hypertension** |
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Term
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Definition
Alpha-2 agonist
-inhibit NE release
-reduced sympathetic output-dec BP
-orally or transdermal patch
-used in treatment of hypertension
-pre anesthetic medication
-side effects: sexual dysfunction, dry mouth, sedation, avoid getting patch too hot!
-rebound hypertension could occur if drug withdrawn abruptly |
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Term
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Definition
Alpha-2 agonist
-inhibit transmitter release
-used in eye: dec intraocular pressure by reducing formation of aqueous humor |
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Term
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Definition
Beta-1 agonist
-Increase force & rate of heart contraction (+ inotropic)
-used in cardiac stress tests
-very short acting (1/2 life=2min)
-Increase AV conduction
-increase renin |
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Term
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Definition
Beta-2 agonist
-cardiac effects less pronounced
-relax respiratory, uterine, blood vessels in skeletal muscle (dec TPR)
-treat Asthma |
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Term
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Definition
Beta-2 agonist
-relaxes uterus (suppresses premature labor)
-given orally or IV |
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Term
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Definition
-stimulates Alpha & Beta receptors, enhances NE release
-similar effect as epinephrine-but less pronounced
-long acting, CNS stimulant, inc HR, inc BP, bronchodilation
-found in many weight loss products-taken off market due to bad side effects & death |
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Term
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Definition
-indirect acting. Increases NE release
-CNS stimulant: inc alertness, dec need for sleep, dec appetite, euphoria, inc motor activity
-tachycardia, hypertension
-psychosis
-Strong contraction of urinary bladder-has been used to treat enuresis |
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Term
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Definition
-inhibits re-uptake of DA and NE
-indirect acting
-shorter acting, more intense than amphetamine
-side effets: HTN, addicting, stroke, arrhythmias, MI, psychosis
-sometimes used as vasoconstrictor for nasopharyngeal surgery. local anesthesia & dec blood flow. |
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Term
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Definition
-indirectly acting. Inc release of NE & DA from nerve terminals
**Pts treated for depression w/ MAO-Inhibitors-injestion of lg amounts may cause severe hypertensive crisis!! |
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Term
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Definition
Dopamine agonist
-D1 at low doses (vasodilation, inc renal blood flow)
-B1 at high concentrations
-treat cardiac shock, increase CO w/o causing vasoconstriction |
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Term
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Definition
dopamine agonist
-Selective D1 receptor agonist
-dilation of vascular beds, dec BP
-used to produce rapid dec in BP w/ severe hypertension |
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Term
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Definition
Phentolamine (regitine)
Phenoxybenzamine (dibenzyline) |
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Term
| Alpha1 Selective Blockers |
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Definition
Prazosin (minipress)
Terazosin (hytrin)
Doxazosin (cardura)
Alfuzosin (uroxatral)
Tamsulosin (Flomax) |
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Term
| Alpha2 Selective Blockers |
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Definition
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Term
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Definition
Propranolol (Inderal)
Timolol (Timoptic) |
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Term
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Definition
Metoprolol (lopressor)
Atenolol (tenormin)
Esmolol (brevibloc)
Betaxolol (betoptic) |
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Term
| Beta-blockers w/ Intrinsic Sympathetic Activity |
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Definition
Pindolol (visken)
Acebutolol (sectral) |
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Term
| Combined Alpha & Beta blockers |
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Definition
Labetalol (normodyne)
Carvedilol (coreg) |
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Term
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Definition
Alpha-receptor blocker
-reversible competitive alpha 1&2 antagonist
-almost never used b/c of amount and severity of side effects (tachycardia, arrhythmias, MI, hypotension, abdominal pain, peptic ulcer exacerbation)
-may be used short-term treatment for hypertensive crisis in pheochromocytoma
-may be used to prevent necrosis if vasoconstrictor (NE) accidently is injected into tissues |
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Term
| Phenoxybenzamine (dibenzyline) |
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Definition
Alpha-receptor blocker
-irreversible antagonist (covalent bond)
-almost never used
-mainly used to treat pheochromocytoma
-tachycardia may occur, hypotension severe if hypovolemic, postrual hypotension, inhibit ejaculation |
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Term
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Definition
Alpha-1 selective blocker
-reversible antagonist
-less likely to increase HR
-relaxes arterial & venus smooth muscle, dec TPR, BP dec, also lack of a2 blockage reduces likelihood of reflex tachycardia
-dec LDL & TG, inc HDL
*1/2 life doubled in CHF (dec dose)
-given 2x a day (not perscribed as much)
-treatment of hypertension
-treatment of Benign prostatic hyperplasia
-Perfect for HTN & BPH together!!
Side effects:
-first does phenomenon (is worst)
-inhibits ejaculation, ED
-dizziness, postural hypotension, nasal stuffiness
**postural hypotension SEVERE if combined w/ Viagra!** |
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Term
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Definition
Alpha-1 selective blocker
-similar to Prazosin
-only given ONCE a day (better choice)
-1st dose phenomenon |
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Term
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Definition
Alpha-1 receptor blocker
-similar to Prazosin
-only given ONCE a day (better choice)
-1st dose phenomenon |
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Term
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Definition
Alpha-1 receptor blocker
-treats BPH
-not as selective as Tamsulosin
-improves urine flow, little effect on BP
-but causes dizziness |
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Term
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Definition
Alpha-1 receptor blocker
-little effect on BP
-treat BPH!! relaxes prostate & sphincer
-side effect: difficulty ejaculating |
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Term
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Definition
Alpha-2 receptor blocker
-herbal preparation
-increases NE release
-BP and HR increase
-"natrual viagra?"
**dangerous to use when have hypertension-will interfere w/ efect of Clonidine** |
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Term
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Definition
Beta-receptor blocker
-competitive antagonist, equal affinity for B1& B2 receptors
-slows HR, dec force of contraction
-slows conduction
-dec renin release
-dec lipolysis & glycogenolysis
-local anesthetic (blocks Na+ channels at higher doses)
-low bioavilibity, high first pass, variable between pts-monitor
-crosses BBB easily, CNS side effects of sedation, depression may occur
-Chronic use: dec BP, dec mortality in post MI pts
-treat hypertension (not 1st choice)
-treat angina
-treat arrhythymias
-treat hyperthyroidism
-dec risk of bleeding in cirrhosis
-revent migranes, reduce tremor, and stage fright
Side effects:
**NOT recommended for Asthmatics**
-bradycardia, rebound htn, mask symptoms of hypoglycemia
*CCB w/ BB might produce additive effects=good |
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Term
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Definition
Beta receptor blocker
-treat Glaucoma (topical)
-absorbed systemically-so should not be used w/ Ashtmatics |
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Term
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Definition
Beta-1 receptor blocker
-Treat Hypertension
-better exercise tolerance than non-selective BB
-increased life expectancy post MI
-migrane prophylaxis
-Risky w/ asthmatics |
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Term
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Definition
Beta-1 receptor blocker
-Treat Hypertension
-better exercise tolerance than non-selective BB
-increased life expectancy post MI
-migrane prophylaxis
-Risky w/ asthmatics |
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Term
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Definition
Beta-1 blocker
-very short duration of action
-must be injected intravenously
-used in urgent situations where rapid effect is needed, or rapid removal of BB effect (HF, bc, Hypotension) |
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Term
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Definition
Beta-1 receptor blocker
-treatment of glaucoma (better choice)
-less likely to cause bronchoconstriction when used in eye than timolol! |
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Term
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Definition
Beta-blocker w/ ISA activity
-non-selective B blocker
-used to treat hypertension and angina
-risk of bradycardia lower
-may not affect plasma lipids |
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Term
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Definition
Beta-blocker w/ ISA activity
-Selective B1 antagonist
-used to treat hypertension and angina
-risk of bradycardia lower
-may not affect plasma lipids |
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Term
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Definition
Combined alpha & beta blocker
-alpha 1 blockade: relaxation of arterial smooth muscle and DEC BP
-B1 blockade: prevents compensatory inc HR (so better than a-blocker alone?)
-treatment of hypertension (orally)
-hypertensive emergencies (intravenously) |
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Term
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Definition
Combined alpha & beta blocker
-non selective beta blocker w/ A1 block
-vasodilation, DEC BP, w/o tachycardia
-treatment of hypertension
-improves morbidity in CHF pts
-seide effects of all B & A blockers=pts don't like the feel |
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