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| Question | Answer |
|---|---|
| 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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