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Midodrine a1 agonist orthostatic hypotension, maintain BP during surgery vasoconstriction
Metaraminol a1 agonist hypotension vasoconstriction/indirectly stimulate NE release
phenylephrine a1 agonist cardiac shock vasoconstriction/increased BP
phenylephrine HCl a1 agonist hypotension vasoconstriction/increased BP
tetryzoline (visine) a1 agonist relieves redness/itchy/watery eyes constricts eye blood vessels
nephazoline (visine A) a1 agonist relieves redness/itchy/watery eyes constricts eye blood vessels
oxymetazoline (visine LR) a1 agonist relieves redness/itchy/watery eyes constricts eye blood vessels
phenylephrine a1 agonist ophthalmic examination (to make eye bigger) contract radial fibers (mydriasis)
mephentermine a1 agonist prevents hypotension from spinal anesthesia Acts DIRECTLY and INDIRECTLY
pheynylephrine a1 agonist nasal decongestant constricts nasal vasculature
nephazoline (visine A) a1 agonist nasal decongestant constricts nasal vasculature
oxymetazoline (visine LR) a1 agonist nasal decongestant constricts nasal vasculature
a1 receptors (7) blood vessels: contract eye: contract radial fibers (dilate) mydriasis glands: increase secretion bladder (internal sphincter): contract uterus: contract penis: ejaculation pilomotor muscle of skin: contract
a1 agonist ADR Predictable: hypotension reflex bradycardia urinary retention
a1 agonist precautions Less efficacy over time b/c desensitization (especially nasal decongestants)
a1 agonist Drug Interactions MAOI (monoamine oxidase inhibitor) TCA (tricyclic antidepressants) Beta blockers
guanabenz a2 agonist hypertension CNS: postsynaptic / decrease SNS activity PNS: presynaptic / decrease NE release
guanfacine a2 agonist hypertension more selective than clonidine for a2
methyldolpa a2 agonist hypertension Prodrug: acts as "false" NE to decrease BP Rec: pregnant hypertension
Clonidine (CATAPRES) a2 agonist hypertension CNS: postsynaptic / decrease SNS activity PNS: presynaptic / decrease NE release
Clonidine (KAPVAY) a2 agonist ADHD stimulate postsynaptic a2a receptors in prefrontal cortex
guanfacine a2 agonist ADHD stimulate postsynaptic a2a receptors in prefrontal cortex
Clonidine (DURACLON) a2 agonist pain management Dorsal horn: decrease release of NE from pain fibers Brain Stem (Locus Cereleus): decrease NE locally
Clonidine (UNLABELED) a2 agonist nicotine/opiate withdrawal decrease excessive NE release from SNS increase peripheral presynaptic a2a
Tizanidine a2 agonist muscle relaxant (spinal disorders) increase presynaptic inhibition of motor neurons
Dexmedomidine a2 agonist ICU sedation CNS postsynaptic: decrease SNS activity Does NOT affect GABA
Lofexidine a2 agonist withdrawal/postmenstrual hot flashes a2a agonist decrease excessive NE release from SNS
Brimonidine (MIRAVASO) a2 agonist tropical treatment for facial erythema rosacea selective a2B blood vessels in skin; vasoconstriction of local blood vessels
Brimonidine (ALPHAGAN) a2 agonist decrease intraocular pressure and open angle gluacoma a2 agonist
Apraclonidine a2 agonist decrease intraocular pressure and open angle gluacoma selective a2 agonist
a2 agonist ADR CNS depression, xerostomia (dry mouth), sexual dysfunction, AV block, constipation, dry eyes ***Caution: dose related withdrawal syndrome Methyldopa ADR: hemolytic anemia & hepatoxicity
a2 agonist Drug Interactions TCA (tricyclic antidepressants) Beta blockers CCBs (Calcium channel blockers) Antihypertensive drgus Alcohol/sedatives
a2 agonist Reversal Agents a2 antagonist regular usage undo analgesic effects of dexmedetomidine in dogs
a2 receptors (5) blood vessels: vasoconstriction PNT: decrease NE release eye: decrease aqueous humor GI: decrease motility CNS: decrease SNS activity/prefrontal cortex firing
B1 receptors (2) Heart: increase contractility, HR, conduction velocity Kidney: increase secretion of renin
Dobutamine b1 selective agonist heart failure/cardiogenic shock Tachycardia ***Tolerance develops due to downregulation/desensitization
B2 receptors (7) blood vessels: relax (dilate) Bladder wall: relax eye: increase aqueous humor Lung bronchi: relax (dilate) uterus: relax Skeletal muscle: increase contractibility heart: effects contractibility, HR, conduction velocity
B3 receptors (3) fat cells bladder wall endothelial cells
B2 agonist SABAS levalbuterol albuterol metoproterenol pirbuterol LAMP "relievers"
B2 agonist LABAS arfomoterol formoterol salmeterol arfo form sal "maintenance"
B2 agonist Ultra-LABAS Vilanterol Indacaterol Olodaterol VIO
B2 agonist Precautions worsening of asthma due to tolerance worsening gluacoma Epilepsy Underlying coronary artery
B2 agonist ADR Predictable: muscle tremors, increase BP, tachycardia, cardiac arrhythmias, restlessness, nervousness, insomnia, Hypokalemia
Terbutaline B2 agonist (SABAS) acute bronchospasm, prevent/manage preterm labor inhibits premature contractions ADR (Predictable): arrhythmia, hypertension, hypokalemia, MI, tachycardia, death
Mirabegron/Vibegron b3 agonist overactive bladder increase bladder capacity by relaxing smooth muscles Hypertension, nasopharyngitis (unpredicted), UTI (unpredicted), headache **not metabolized by CYP3A4, 2D6, or 2C9, lower BBB protection
Isoproterenol Non-selective Beta agonist used in EMERGENCIES for pt w/ bradycardia/heart block lower peripheral vascular resistance, increase cardia output ADR (predictable) palpitations, tachycardia, headache, flushing cardiac ischemia/arrhythmias
Epinephrine Non-selective a and B agonist increase HR, decrease bleeding ADR: cardiac arrhythmia, tachycardia, hypertensive crisis, cerebral hemorrhage, tremor Drug Interactions (increase): MAOI, TCA, cocaine (decrease): aB blocker
Norepinephrine Non-selective a and B agonist (no B2) hypotension from cardiovascular shock ADR: Vasoconstriction
Dopamine 1 blood vessels: relax (dilate)
Dopamine 2 pituitary: decrease prolactin secretion
Fenoldopam Selective D1 agonist acute severe hypertension vasodilation of renal/peripheral blood vessels ADR (Predictable): hypotension, tachybardia, hypokalemia
Bromocriptine D2 agonist Acromegaly, hyperprolactinemia, parkinsonism, type 2 diabetes Pituitary: inhibit prolactin secretion CNS nigrostriatal: restore motor function ADR (Unpredicted): cardiac valve/pleural fibrosis MI, stroke, seizures
Dopamine D1,2/A1/B1 Agonist cardiogenic shock from low cardiac output dilate renal coronary/mesenteric arteries (low dose): d1 renal vasodilation d2 decrease NE release (mid dose): increase HR (high dose): vasoconstriction DI: a/B blockers/MAOI
Clinical use of amphetamines/methylphenidate narcolepsy (all works except methamphetamine) obesity (short-term only)
Amphetamines/Methylphenidate Drug Interactions/ADR DI: Sympathomimetic drugs, MAOI, Selective serotonin reuptake inhibitors (SSRI) ADR: CNS - anxiety, panic attack, hallucinations, schizophrenia CVS - hypertension, cardiac death/stroke skeletal muscle tremors growth retardation
Amphetamines Amphetamine Dextroamphetamine Methamphetamine Amphetamine Mixture Lisdexamfetamine Dimesylate/Vyvanse (Prodrug - slows hydrolysis) ***Others cause increase DA and NE Also Mixed-Acting Sympathomimetic
Methylphenidates Concerta Daytrana Methylin (syrup/chewable) Focalin Focalin XR Quillivant XR QuilliChew ER Adhansia XR Jornay PM Metadate CD Aptensio XR Azstarys
Lisdexamfetamine Dimesylate/Vyvanse Amphetamine (indirect sympathomimetic) Prodrug - slows hydrolysis
Ritalin Methylphenidates (indirect sympathomimetic) Immediate release
Ritalin SR Methylphenidates (indirect sympathomimetic) Extended release
Ritalin LA Methylphenidates (indirect sympathomimetic) Extended release with initial IR dose
Concerta Methylphenidates (indirect sympathomimetic) new delivery system with multiple compartments for slow release taken once daily
Daytrana Methylphenidates (indirect sympathomimetic) Transdermal absorption
Methylin Methylphenidates (indirect sympathomimetic) Syrup, chewable immediate release
Jornay PM Methylphenidates (indirect sympathomimetic) Taken at night
Metadate CD Methylphenidates (indirect sympathomimetic) Contains both IR and ER beads Taken once daily
Aptensio XR Methylphenidates (indirect sympathomimetic) Contains both IR and ER beads
Azstarys Methylphenidates (indirect sympathomimetic) Dexmethylphenidate (IR) and Serdexmethylphenidate (Prodrug)
Atomoxetine (Strattera) Selective NE Reuptake Inhibitor ADHD Inhibit presynaptic NET, does not increase DA ADR: nausea, anorexia, increase BP, insomnia, suicidality, metabolize by CYP2D6 C/I: Glaucoma, MAOI, tachycardia
Qelbree (Viloxazine ER) Selective NE Reuptake Inhibitor/Mixed-acting Sympathomimetic SNRI and antagonist/agonst of 5-HT. Does not increase DA ADR: suicidal, increase HR/BP, similar atomoxetine
Anorectic Drugs Amphetamine Congeners, Phentermine/Topiramate, Diethylpropion, Methamphetamines, Mazindol Obesity Short-term appetite suppressant Tolerance if prolong use
Narcolepsy Amphetamines Dextroamphetamines Methylphenidates Modafinil (CIV) Armodafinil (CIV)
Modafinil (CIV) Narcolepsy Drug (indirect sympathomimetic) Narcolepsy Inhibit NA, DA uptake Increases 5-HT Decreases GABA in CNS Headache, nausea, life-threatening rashes, arrhythmias, hypertension
Cocaine Indirect sympathomimetics Local Anesthetic for upper respiratory tract Block reuptake of NE, DA, and 5-HT Anxiety, agitation, hallucination, hyperthermia, arrhythmias, hypertension, hemorrhagic stroke
Pseudoephedrine Mixed-Acting Sympathomimetic Drug Nasal Decongestant increase NE release/weak a1 and B agonist
Ephedrine HCl/Ephedrine Sulfate Mixed-Acting Sympathomimetic Drug Intraoperative hypotension increase NE release/weak a1 and B agonist
Metaraminol Mixed-Acting Sympathomimetic Drug Prevent hypotension from spinal anesthesia increase NE release/a1 agonist
Mephenteramine Mixed-Acting Sympathomimetic Drug Prevent hypotension from spinal anesthesia increase NE release/a1 agonist
Sympathomimetics drugs that mimics the actions of epinephrine or norepinephrine Direct acting = directly interacts with and activates Epi/NE Indirect acting: actions depends on their ability to enhance the actions of MOAIs, COMT inhibitors, etc
Indirect-acting/Mixed-acting Sympathomimetics Indirect Acting: these drugs increase synaptic concentrations of endogenous neurotransmitters Some also have some direct effects and are called “mixed acting sympathomimetics”
Sympatholytics Direct acting: Bind to adrenergic receptors and prevent their activation by endogenous catecholamines Indirect acting: Act indirectly by inhibiting synthesis, release, or reuptake of NE
Metyrosine (Demser) Indirect Sympatholytics Hypertension Affect NE synthesis by inhibiting tyrosine hydroxylase hypotension, diarrhea, nasal stuffiness
Reserpine Indirect Sympatholytics Hypertension Irreversibly block catecholamine uptake in storage granules Depletion of DA and serotonin, sedation, psychotic depression
Indirect-acting Sympatholytics Clonidine, methyldopa, guanfacine, guanabenz a2 agonist that decrease NE release
Indirect-acting Sympatholytics Guanethidine, bretylium Affect NE release; vesicular fusion blocker
Phenotolamine Non-Selective a1/a2 Blocker Regitine: Pheochromocytoma/hypertensive crisis. Reverse toxicity of a agonist Oraverse: Reverse local anesthesia Block a1 receptor, inhibit vasoconstriction, lower BP
Phenoxybenzamine Non-Selective a1/a2 Blocker Dibenzyline: Hypertension due to pheochromocytoma/sympathomimetics
Doxazosin Selective a1 blocker hypertension/BPH blocks a1b, relax prostate wall/internal sphincter
Praozosin Selective a1 blocker hypertension/BPH blocks a1b, relax prostate wall/internal sphincter
Terazosin Selective a1 blocker hypertension/BPH blocks a1b then relax prostate wall/internal sphincter
Afluzosin Selective a1 blocker BPH blocks a1b then selective accumulate in prostate tissue. No orthostatic hypotension (fainting)
Tamsulosin Selective a1 blocker BPH blocks a1b then lower chance of orthostatic hypotension (fainting)
Silodosin Selective a1 blocker BPH blocks a1b then lower chance of orthostatic hypotension (fainting)
Yohimbine Selective a2 blocker ED, hypotension, weight loss blocks a2 receptors to increase NE release, raise BP/HR anxiety, increased BP if NET blocked
ADR of a Blockade Orthostatic hypotension (decreased BP -> fainting) Nasal congestion Inhibition of ejaculation Miosis Reflex tachycardia (stimulates B1 receptors) Intraoperative Floppy Iris Syndrome during cataract surgery Priapism
Atipamezole Selective a2 blocker Reverses analgesia from dexmedetomidine
Nonselective Beta Blocker (1st gen) Nadolol Propranolol Labetalol Carvedilol Sotalol "NaPLaCS"
B1 Selective (2nd gen/Cardioselective) Metoprolol Bisoprolol Esmolol Atenolol Nebivolol "MetBEAN"
Nonselective Beta Blocker (1st gen) Indications Hypertension Angina Congestive Heart Failure Supraventricular tachycardia Open Angle Glaucoma Anxiety/alcohol withdrawal Migraine prophylaxis
Nonselective Beta Blocker (1st gen) MOA 1.Inhibits renin activation + PNS effects. 2.Decrease O2 demand. 3.Decrease O2 demand and risk of ventricular arrhythmias. 4.Slow AV conduction. 5.↓ aqueous humor. 6.↓ SNS response. Block β1 to normalize vascular ton.
Acebutolol Propranolol Membrane Stabilizer (Beta Blocker) Inhibits Na+ channels to stabilize membrane Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Acebutolol Pindolol Intrinsic Sympathomimetic Partial agonist of B receptors. Good for asthma Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Acebutolol Sotalol Potassium blockers Prolongs action potential duration Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Carvedilol B blocker + a1 antagonist (vasodilator) Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Labetalol B blocker + a1 antagonist (vasodilator) Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Nevibolol Blocker + NO activity (vasodilator) Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma ***increases NO for vasodilation
Cateolol Blocker + NO activity (vasodilator) Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Celiprolol Blocker + NO activity (vasodilator) Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Bucindolol Blocker + B2 Agonist activity (vasodilator) Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Carteolol Blocker + B2 Agonist activity (vasodilator) Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Celiprolol Blocker + B2 Agonist activity (vasodilator) Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Betaxolol Blocker + Ca2+ Channel Blocking activity (vasodilator) Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Carvedilol Blocker + Ca2+ Channel Blocking activity (vasodilator) Hyperthyroidism. Hyperkalemia since less K+ uptake. Loss libido. Depression. Can result in hyper or hypoglycemia. Don’t use with pheochromocytoma
Timolol Glaucoma B Blocker Glaucoma Treat increased intraocular pressure from glaucoma absorption into circulation -> head/respiratory ADR
Carteolol Glaucoma B Blocker Glaucoma Treat increased intraocular pressure from glaucoma absorption into circulation -> head/respiratory ADR
Metripranolol Glaucoma B Blocker Glaucoma Treat increased intraocular pressure from glaucoma absorption into circulation -> head/respiratory ADR
Levobunolol Glaucoma B Blocker Glaucoma Treat increased intraocular pressure from glaucoma absorption into circulation -> head/respiratory ADR
Betaxolol Glaucoma B Blocker Glaucoma Treat increased intraocular pressure from glaucoma absorption into circulation -> head/respiratory ADR
Pilocarpine Direct Cholinergic Drugs Glaucoma, Dry Mouth Short Acting - binds to active sites by hydrogen bonds Long Acting - bond between ester and hydroxyl group DUMBBELLS
Bethanechol Direct Cholinergic Drugs Postoperative Ileus, Urinary retention Short Acting - binds to active sites by hydrogen bonds Long Acting - bond between ester and hydroxyl group DUMBBELLS
Carbachol Direct Cholinergic Drugs Glaucoma Short Acting - binds to active sites by hydrogen bonds Long Acting - bond between ester and hydroxyl group DUMBBELLS
Cevimeline Direct Cholinergic Drugs Dry Mouth Short Acting - binds to active sites by hydrogen bonds Long Acting - bond between ester and hydroxyl group DUMBBELLS
Created by: jliu913
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