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Neuropharmacology 1
Sympathomimetic Drugs (Direct/Indirect /Mixed)
| Drug | Action | Indication | MOA |
|---|---|---|---|
| Midodrine (promatine) | Direct Sympathomimetics Systemic Alpha 1 Agonist PO | Hypotension (BP for during surgery) | vasoconstriction |
| Metaraminol (aramine) | Direct Sympathomimetics Systemic Alpha 1 Agonist IM, Subq, IV | Hypotensive state; Atrial tachycardia | Vasoconstriction/stimulate release of NE |
| Phenylephrine (neo-synephrine) | Direct Sympathomimetics Systemic Alpha 1 Agonist IV | Cardiac Shock | Vasoconstriction (increase BP; increase venous return |
| Phenylephrine Hydrochloride (Biorphen) | Direct Sympathomimetics Systemic Alpha 1 Agonist IV | Hypotension (from anesthesia) | Vasoconstriction (increase BP; increase venous return |
| Mephentermine (Wyamine Sulfate) | Direct Sympathomimetics Systemic Alpha 1 Agonist IM | Prevent Hypotension which result from spinal anesthesia | Directly and Indirectly |
| Phenylephrine (neo-synephrine) | Direct Sympathomimetics Ophthalmic Alpha 1 Agonist Eye Drop | MYDRIASIS | Contract RADIAL (outer) fibers of iris |
| Nephazoline (NAPHCON w/ pheniramine= Visine-A) | Direct Sympathomimetics Ophthalmic Alpha 1 Agonist Eye Drop | Relieve redness/puffy/ also for colds, allergies, and eye irritants used for itchy/watering eyes | Constrict ocular blood vessels |
| Oxymetazoline (Visine L.R.) | Direct Sympathomimetics Ophthalmic Alpha 1 Agonist Eye Drop | Relieve redness/puffy/ also for colds, allergies, and eye irritants used for itchy/watering eyes | Constrict ocular blood vessels |
| Tetryzoline (Visine) | Direct Sympathomimetics Ophthalmic Alpha 1 Agonist Eye Drop | Relieve redness/puffy/ also for colds, allergies, and eye irritants used for itchy/watering eyes | Constrict ocular blood vessels |
| Phenylephrine (neo-synephrine) | Direct Sympathomimetics Nasal Alpha 1 Agonist Nasal Spray | Nasal Decongestant | Constrict Nasal vasculature and mucosa |
| Nephazoline (privine) | Direct Sympathomimetics Nasal Alpha 1 Agonist Nasal Spray | Nasal Decongestant | Constrict Nasal vasculature and mucosa |
| Oxymetazoline (Afrin) | Direct Sympathomimetics Nasal Alpha 1 Agonist Nasal Spray | Nasal Decongestant | Constrict Nasal vasculature and mucosa) |
| Alpha 1 Agonist Issues | ADR(Predictable/to well): Hypertension, reflex bradycardia; urinary retention | Drug Interactions: MAOIs-activate; TCAs-affect alpha 1 receptor in brain; Beta blockers-counter act | Precautions: Less efficacy over time due to receptor desensitization (especially for nasal decongestants) |
| Clonidine (Catapres) | Direct Sympathomimetics Systemic Alpha 2 Agonist | Hypertension (off label ADHD) Reduce menopausal hot flashes (transdermal application) | CNS Postsynaptic receptor (DECREASE SNS ACTIVITY) ; PNS Presynaptic receptor (DECREASE NE release) |
| Clonidine (Kapvay) | Direct Sympathomimetics Systemic Alpha 2 Agonist | ADHD | Stimulate Prefrontal cortex Postsynaptic alpha 2 receptors (decreases the basal firing rate of neurons (PFC adrenergic) improving cog. function; improve working memory, behavioral inhib, attention, focus, planning, decrease hyper and distract. |
| Clonidine (Duraclon) | Direct Sympathomimetics Systemic Alpha 2 Agonist | Pain Management | Dorsal Horn: decrease release of NT from pain fiber and inhibit ascending nociceptive transmission Brain Stem (Locus Ceruleus): Suppress pain transmission coming from dorsal horn , decreases NE locally |
| Clonidine ( Unlabeled use) | Direct Sympathomimetics Systemic Alpha 2 Agonist | Nicotine & Opiate Withdrawal | Activation of peripheral presynaptic alpha 2 receptors (decrease excessive NE release from SNS nerves that are associated with withdrawal of nicotine or opiates) |
| Clonidine (other unlabeled use) | Direct Sympathomimetics Systemic Alpha 2 Agonist | Continuous Admiration ( Transdermal patch) | Reducing Diarrhea (diabetic patients with autonomic neuropathy) |
| Guanabenz (Wytensin) | Direct Sympathomimetics Systemic Alpha 2 Agonist (Similar to Clonidine Catapres) | Hypertension | CNS Postsynaptic receptor (decrease SNS activity) PNS Presynaptic receptor (decrease NE release) |
| Guanfacine (Tenex, Intuniv) | Direct Sympathomimetics Systemic Alpha 2 Agonist (Similar to Clonidine Catapres) | Hypertension; | CNS Postsynaptic receptor (decrease SNS activity) PNS Presynaptic receptor (decrease NE release) ; *more selective than clonidine to the alpha 2 receptor |
| Methyldopa (Aldomet) | Direct Sympathomimetics Systemic Alpha 2 Agonist (Similar to Clonidine Catapres) | Hypertension (preferred to treat during pregnancy) | CNS Postsynaptic (dec. SNS activity) PNS Presynaptic (dec. NE release) ; *acts also as a "False Transmiter"=weak agonist of adrenergic receptor); prodrug metab. to alpha methyl NE (agonist) which is stored then released from storage instead of NE) |
| Guanfacine (Tenex, Intuniv) | Direct Sympathomimetics Systemic Alpha 2 Agonist Similar to Clonidine Kapvay | ADHD | Stimulate Prefrontal cortex Postsynaptic alpha 2 receptors (decreases the basal firing rate of neurons (PFC adrenergic) improving cog. function; improve working memory, behavioral inhib, attention, focus, planning, decrease hyper and distract. |
| Tizanidine (zanaflex) | Direct Sympathomimetics Systemic Alpha 2 Agonist | Muscle Relaxant (treat spasticity asoc. with cerebral/spinal disorders | Agonist with similar properties with clonidine; increase presynaptic inhibition of motor neurons |
| Dexmedetomidine (Precedex) | Direct Sympathomimetics Systemic Alpha 2 Agonist | Sedation (in ICU /procedures) | CNS Postsynaptic receptor (decrease SNS activity) ; Decrease activity of Noradrenergic neurons in the locus ceruleus in the brain stem; notable sedative due to not affecting GABA activity |
| Lofexidine (Lucemyra) | Direct Sympathomimetics Systemic Alpha 2 Agonist | Opioid, Alcohol Withdrawal Postmenstrual Hot Flashes | Decrease excessive NE release from SNS nerves that are associated with withdrawal of opiates; No effect on drug cravings |
| Brimonidine (MIRVASO) | Direct Sympathomimetics Topical Alpha 2 Agonist | Topical treatment of persistent facial erythema of rosacea in adults 18 yrs + | Receptor Agonist Selective activation of receptors in blood vessels in skin leading to vasoconstriction of local blood vessels (ADR caution in use with patient with severe/uncontrolled CVD); Can cross blood brain barrier and cause hypotension and sedation |
| Brimonidine (ALPHAGAN) | Direct Sympathomimetics Topical Alpha 2 Agonist | Administered OCULARLY to lower intraocular pressure in patients with ocular hypertension or open-angle glaucoma-decrease aq humor) | Receptor agonist (ADR caution in use with patient with severe/uncontrolled CVD) ; Can cross blood brain barrier and cause hypotension and sedation |
| Apraclonidine (Iopidine) | Direct Sympathomimetics Topical Alpha 2 Agonist | Topically to reduce intraOCULAR pressure ; open angle glaucoma-need to reduce aq humor) | Selective alpha receptor agonist ADR (predictable): Dry mouth ADR (unpredictable): allergic conjunctivitis and visual disturbances |
| Alpha 2 Agonist Issues | ADR : CNS depression; xerostomia (dry mouth), sex dysfunction, AV block, constipation, dry eyes Methyldopa: Hemolytic anemia and Hepatotoxicity (need periodic liver function tests LFTs, blood counts, Coombs test before treatment and periodically) | Drug interactions: TCA; beta blockers; calcium; CCB (calcium channel blockers); antihypertensive drugs; alcohol and other sedatives | Reversal Agents: Alpha 2 antagonists like Atipamezole (Antisedan); regularly to undo analgesic effects of dexmedetomidine in dogs) |
| Dobutamine (Dobutrex) | Direct Sympathomimetics Selective Beta 1 Agonist | Heart Failure and Cardiogenic Shock | Positive inotropic effect (increased CO) Precaution: tolerance develops due to down regulation and desensitization of receptors) |
| Albuterol (Proair; Proventil; Vospire) | Direct Sympathomimetics SABA (Short Acting Beta 2 Agonist) | 2-6 hrs Relief of acute asthma symptoms and exacerbations (quick relief- ”relievers”) May be used as monotherapy Taken before exercise to prevent exercise induced bronchospasm (EIB) | activate pulmonary receptors that relax bronchial smooth muscle and decrease airway resistance. suppress the release of leukotrienes and histamine from mast cells in lung tissue, enhance mucociliary function, and decrease microvascular permeability |
| Levalbuterol (Xopenex) | Direct Sympathomimetics SABA (Short Acting Beta 2 Agonist) | 2-6 hrs Relief of acute asthma symptoms and exacerbations (quick relief- ”relievers”) May be used as monotherapy Taken before exercise to prevent exercise induced bronchospasm (EIB) | activate pulmonary receptors that relax bronchial smooth muscle and decrease airway resistance. suppress the release of leukotrienes and histamine from mast cells in lung tissue, enhance mucociliary function, and decrease microvascular permeability |
| Metoproterenol (Alupent) | Direct Sympathomimetics SABA (Short Acting Beta 2 Agonist) | 2-6 hrs Relief of acute asthma symptoms and exacerbations (quick relief- ”relievers”) May be used as monotherapy Taken before exercise to prevent exercise induced bronchospasm (EIB) | activate pulmonary receptors that relax bronchial smooth muscle and decrease airway resistance. suppress the release of leukotrienes and histamine from mast cells in lung tissue, enhance mucociliary function, and decrease microvascular permeability |
| Pributerol (Maxair) | Direct Sympathomimetics SABA (Short Acting Beta 2 Agonist) | 2-6 hrs Relief of acute asthma symptoms and exacerbations (quick relief- ”relievers”) May be used as monotherapy Taken before exercise to prevent exercise induced bronchospasm (EIB) | activate pulmonary receptors that relax bronchial smooth muscle and decrease airway resistance. suppress the release of leukotrienes and histamine from mast cells in lung tissue, enhance mucociliary function, and decrease microvascular permeability |
| Arformoterol (Brovana) | Direct Sympathomimetics LABA (Long Acting Beta 2 Agonist) | 12 hrs Long Term prevention of asthma symptoms (maintenance) Not used as monotherapy, must be given with concomitant anti-inflammatory drug | activate pulmonary receptors that relax bronchial smooth muscle and decrease airway resistance. suppress the release of leukotrienes and histamine from mast cells in lung tissue, enhance mucociliary function, and decrease microvascular permeability |
| Formoterol (Fordil) -Symbicort with Budesonide | Direct Sympathomimetics LABA (Long Acting Beta 2 Agonist) | 12 hrs Long Term prevention of asthma symptoms (maintenance) Not used as monotherapy, must be given with concomitant anti-inflammatory drug (SYMBICORT FOR ACUTE ASTHMA AND COPD) | activate pulmonary receptors that relax bronchial smooth muscle and decrease airway resistance. suppress the release of leukotrienes and histamine from mast cells in lung tissue, enhance mucociliary function, and decrease microvascular permeability |
| Salmeterol (Serevent) - Advair and Airduo with Fluticasone | Direct Sympathomimetics LABA (Long Acting Beta 2 Agonist) | 12 hrs Long Term prevention of asthma symptoms (maintenance) Not used as monotherapy, must be given with concomitant anti-inflammatory drug (ADVAIR FOR ACUTE ASTHMA) | activate pulmonary receptors that relax bronchial smooth muscle and decrease airway resistance. suppress the release of leukotrienes and histamine from mast cells in lung tissue, enhance mucociliary function, and decrease microvascular permeability |
| Olodaterol (Striverdi Respimat) | Direct Sympathomimetics Ultra-LABA (Ultra Long Acting Beta 2 Agonist) | 24 hrs Long Term prevention of asthma symptoms (maintenance) Not used as monotherapy, must be given with concomitant anti-inflammatory drug | activate pulmonary receptors that relax bronchial smooth muscle and decrease airway resistance. suppress the release of leukotrienes and histamine from mast cells in lung tissue, enhance mucociliary function, and decrease microvascular permeability |
| Indacaterol (Arcapta) | Direct Sympathomimetics Ultra-LABA (Ultra Long Acting Beta 2 Agonist) | 24 hrs Long Term prevention of asthma symptoms (maintenance) Not used as monotherapy, must be given with concomitant anti-inflammatory drug | activate pulmonary receptors that relax bronchial smooth muscle and decrease airway resistance. suppress the release of leukotrienes and histamine from mast cells in lung tissue, enhance mucociliary function, and decrease microvascular permeability |
| Vilanterol (Breo Ellipta with fluticasone) | Direct Sympathomimetics Ultra-LABA (Ultra Long Acting Beta 2 Agonist) | 24 hrs Long Term prevention of asthma symptoms (maintenance) Not used as monotherapy, must be given with concomitant anti-inflammatory drug | activate pulmonary receptors that relax bronchial smooth muscle and decrease airway resistance. suppress the release of leukotrienes and histamine from mast cells in lung tissue, enhance mucociliary function, and decrease microvascular permeability |
| B2 Agonist Precautions | Precautions: worsening of asthma symptoms due to tolerance (with overuse, downregulation of b2 receptor) and paradoxical effect; worsen glaucoma; epilepsy (receptor may stimulate CNS); patients with underlying Coronary artery disease, arrhythmias | ADR (less likely with inhalation) Predictable: Muscle tremor, increase blood pressure tachycardia, cardiac arrhythmias, restlessness, nervousness, insomnia | Also Hypokalemia (especially important for patients taking digoxin or diuretics) due to increase in K+ excretion; (decrease in blood stream) |
| Terbutaline (Brethine) | Direct Sympathomimetics SABA (Short Acting Beta 2 Agonist) | Acute Bronchospasm (no longer); main as injection to prevent and mange preterm labor (tocolytic) | Inhibit premature contractions ADR: Arrhythmia, hypertension, hypokalemia, MI, tachycardia, death; potential maternal issues such as heart problems and death |
| Mirabegron (Myrbetriq) | Direct Sympathomimetics Beta 3 Agonist (Begron) | Treatment of overactive bladder (symptoms of urge urinary incontinence, urgency and urinary frequency) | Increases bladder capacity by relaxing the detrusor smooth muscle by the activation of receptors ;ADR: hypertension, headache (lower BBB penetration), Unpredicted: nasopharyngitis, UTI, |
| Vibegron (Gemtesa) | Direct Sympathomimetics Beta 3 Agonist (Begron) | Treatment of overactive bladder (symptoms of urge urinary incontinence, urgency and urinary frequency) | Increases bladder capacity by relaxing the detrusor smooth muscle by the activation of receptors ;ADR: hypertension, headache (lower BBB penetration), Unpredicted: nasopharyngitis, UTI; vigegron not metabolized by CYP3A4, 2D6, or 2C9 |
| Isoproterenol (Isuprel) | Direct Sympathomimetics Non Selective Beta Agonist | Used in emergencies to stimulate heart rate in patients with bradycardia or heart block ADR: Predictable-palpitations, tachycardia, headache, flushing, headache (receptors in brain); Cardiac ischemia and arrhythmias may occur | Potent agonist with very low affinity for alpha receptors; lowers peripheral vascular resistance; increases cardiac output |
| Epinephrine (Adrenalin, Epipen, Auvi-Q) | Direct Sympathomimetics Non Selective Alpha and Beta Agonists | Bradycardia (unresponsive to atropine); Cardiac arrest (intracardiac injection); Decrease superficial bleeding (vasoconstriction); Hypotension shock resistant to fluid restoration therapy; prolong action of local anesthetics; severe allergic reactions | severe allergic reactions: dilate bronchi, inhibit mast cell release of histamines and leukotrienes Interactions: Increase Effect: MAO inhibitors; cocaine; TCA; Hyperthyroidism; Effects Decrease: alpha and beta blockers; ADR: to much SNS activity |
| Norepinephrine (Noradrenalin, levophed) | Direct Sympathomimetics Non Selective Alpha and Beta Agonist (except B2) | Hypotension associated with cardiovascular shock that does not respond to fluid replacement, dopamine or dobutamine | Nonselective α and β agonist (α1 = α2 > β1); ADR: If extravasation occurs, to prevent sloughing/necrosis in peripheral ischemic areas (because of vasoconstriction), infiltrate area with phentolamine. |
| Fenoldopam (Corlopam) | Direct Sympathomimetics Selective D1 Agonist | Acute severe hypertension (short term treatment) ADR: (Predictable) Dose-related hypotension, tachycardia, hypokalemia (due to some affinity to beta adrenergic receptors) | vasodilation of renal and other peripheral blood vessels decreases vascular resistance and maintains renal blood flow to reduce risk of renal failure 6x potent than dopamine in producing renal vasodilation |
| Bromocriptine (Parlodel) | Direct Sympathomimetics D2 Agonist ADR: cardiac valve and pleural fibrosis (unpredicted) ; MI, stroke, seizures | Acromegaly(Hypersecretion of growth hormone due to adenoma (bromocriptine causes paradoxical decrease in GH)); Hyperprolactinemia (to decrease prolactin) Parkinsonism Type-2 diabetes mellitus (control insulin release) | Agonist in pituitary gland (inhibit prolactin hypersecretion); Agonist in CNS nigrostriatal pathway (restore motor function; Parkinson's); affect circadian rhythms |
| Dopamine (Inotropin) DI: α blockers reduce vasoconstrict caused by HD dopamine; β block reduce cardiac effects of dop; monoamine oxidase inhibitors: raise hypertens crisis due to excessive cardiac stim and vasoconstrict | Direct Sympathomimetics D1 and D2 receptor agonist and B1 and A1 receptor agonist (dose- dependent) | Adjunct in treatment of cardiogenic shock associated with low cardiac output (CO) and compromised renal function Given by IV infusion due to rapid metabolism by MAO and COMT | Dilates renal coronary and mesenteric arteries; Low dose (D1: renal vasodilation ; D2: presynaptic D2 recep(decrease NE release); Inter: Cardiac B1 receptor (increase HR, contract. and CO); HD:stimulate vascular alpha recep.(vasoconstrict to maintain BP) |
| Amphetamine (Benzedrine) | Indirect Acting Sympathomimetics Racemic mixture of D and L- amphetamine | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE by blocking transporters; promotes relase of monoamine neurotrasmitters (NE, DA, 5-HT); weak inhibitor of MAO; act as a direct agonist on central 5-HT receptors |
| Dextroamphetamine (Dexedrine) | Indirect Acting Sympathomimetics D-Isomer of Ampetamine Greater CNS stimulating activity (less PNS) | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE by blocking transporters; promotes relase of monoamine neurotrasmitters (NE, DA, 5-HT); weak inhibitor of MAO; act as a direct agonist on central 5-HT receptors |
| Methamphetamine (Desoxyn) | Indirect Acting Sympathomimetics Levo- and dextro-methamphetamine More CNS stimulating effects | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE by blocking transporters; promotes relase of monoamine neurotrasmitters (NE, DA, 5-HT); weak inhibitor of MAO; act as a direct agonist on central 5-HT receptors |
| Amphetamine mixture (Adderall) | Sympathomimetics combination of amphetamine and dextroamphetamine | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE by blocking transporters; promotes relase of monoamine neurotrasmitters (NE, DA, 5-HT); weak inhibitor of MAO; act as a direct agonist on central 5-HT receptors |
| Lisdexamfetamine Dimesylate (Vyvanse) | Indirect Sympathomimetics Prodrug of Dextroamphetamine Lessen drug abuse potential | ADHD; Additional Uses: (slow hydrolysis ) Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | (Prodrug converted to amphetamines) Inhibit reuptake of DA and NE by blocking transporters; promotes relase of monoamine neurotrasmitters (NE, DA, 5-HT); weak inhibitor of MAO; act as a direct agonist on central 5-HT receptors |
| Ritalin (IR,ER,ER with intial IR dose) | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE |
| Concerta (ER with intial IR dose) | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE; Once a day in am for 12 hours; increase privacy(taken at home and less fluctuation of blood level) |
| Daytrana (Film, ER) | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE |
| Methylin (solution, tablet, chew) | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE |
| Focalin (dexmethylphenidate, Focalin XR Sprinkles) | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Dextro- methylphenidate, may provide better effect than racemic dextro- and levo methylphenidate formulations (ie Ritalin) | Inhibit reuptake of DA and NE |
| Quillivant XR; Quillichew ER | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE |
| Adhansia XR | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE |
| Jornay PM | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE; Night administration (6:30-9:30PM); starts working in AM (Delayed for 10 hours) great for kids; |
| Metadate CD | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE; CD is 1 per day composed of two parts an IR and ER component (different %) |
| Aptensio XR | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE; XR is composed of two parts an IR and ER component (different %) |
| Azstarys | Indirect Sympathomimetics Methylphenidate | ADHD; Additional Uses: Narcolepsy (IR only and not methamphetamine; Increase NE); Obesity (short-term; increase NE) | Inhibit reuptake of DA and NE; combination of IR Dexmethylphenidate followed by prodrug serdexmethylphenidate which is slowly released (converts to dexmethylphenidate) |
| Amphetamines and Methylphenidate Issues | Drug Interactions: Sympathomimetic drugs; MAOI (hypertensive crisis); SSRI (risk of serotonin syndrome) | ADR: CNS : anxiety, panic attack (increased NE); hallucinations/paranoid delusions (Increased DA) CVS (hypertension, MI, stroke) Skeletal muscles tremors Growth retardation in children* | Contraindication: MAOI; Glaucoma; anxiety; inhaled anesthetics; advanced arteriosclerosis; moderate/severe hypertension Precaution: uncontrolled hypertension; seizures Warning: drug dependency; avoid abrupt discontinuation for patients taking for longx |
| Amphetamines and Methylphenidate Issues | Treatment of OD: Hallucinations and delusions (treat with antipsychotics ) Severe Hypertension (use alpha-blocker i.e phentolamine) | Convulsions,coma, cerebral hemorrhage in fatal overdose (acidify the urine with ammonium chloride to increase amphetamine excretion) | Warnings: potential for drug dependency; avoid abrupt discontinuation in patients have received for prolonged periods Sudden Cardiac Death, stroke, MI |
| Atomoxetine (strattera) | Indirect Sympathomimetics SNRI (Selective Norepinephrine Reuptake Inhibitors) | ADHD (**NON-STIMULANT/NON-CONTROLLED**) | SNRI inhibits the pre-synaptic NE transporter (NET) (Dosen't increase DA in striatum & nucleus accumbens=no dependency (also signifigantly slower onset than stimulants 2-4 weeks vs hrs**); Little insomnia |
| Qelbree (viloxazine ER Caps) | Indirect Sympathomimetics SNRI (Selective Norepinephrine Reuptake Inhibitors) | ADHD (**NON-STIMULANT/NON-CONTROLLED**) Pediatric Patients 6-17 | SSRI ANTAGONIST activity at serotonin receptor (5-HT2B) and AGONIST activity at (5-HT2C) |
| SSRI Issues | ADR: Nausea, anorexia, increased blood pressure, fatigue, sedation, severe liver injury, suicidality; mild insomnia; METABOLIZED BY CYP2D6 (higher levels in poor metabolizers**) | Contraindications: Glaucoma (narrow angle-B2 receptor in eye=more aq humor); MAOIs w/ last 2 weeks; pheochromocytoma (tumor on adrenal medulla=more NE); caution patients in tachycardia, hypertension, CV disease | Precautions: Oral/IV albuterol (and other systemic B2 agonsists); CYP2D6 inhibitors |
| Dosing Considerations for all ADHD Drugs | Use lowest effective dose; start with low initial dose and gradually titrate upward until symptoms improve or SE appear; monitor for insomnia and possible growth suppression | Give during or after meals; Drug holidays (patient talk off on occasion; especially pediatrics for summer vacation); periodically assessed during interrupted doses | Shorter Duration of action products (Advantage: avoid loss of appetite or difficult falling asleep in PM; Disadvantage: if effect is needed in PM; Compliance problem with midday and late PM dosing; blood level fluctuations) |
| (Phentermine(Fastin) | Amphetamine Congeners Indirect Sympathomimetics Anorectic Drugs | appetite suppressants or anorexiants | Short-term use for caloric restriction and behavioral modification. Monotherapy only with treatments such as exercise. Prolonged use not recommended. Tolerance after several weeks. If tolerance to anorexigenic effect develops, discontinue drug |
| Phentermine/Topiramate (QSYMIA) | Amphetamine Congeners Indirect Sympathomimetics Anorectic Drugs | appetite suppressants or anorexiants | Short-term use for caloric restriction and behavioral modification. Monotherapy only with treatments such as exercise. Prolonged use not recommended. Tolerance after several weeks. If tolerance to anorexigenic effect develops, discontinue drug |
| Diethylproprion (Tenuate) | Amphetamine Congeners Indirect Sympathomimetics Anorectic Drugs | appetite suppressants or anorexiants | Short-term use for caloric restriction and behavioral modification. Monotherapy only with treatments such as exercise. Prolonged use not recommended. Tolerance after several weeks. If tolerance to anorexigenic effect develops, discontinue drug |
| Methamphetamines | Indirect Sympathomimetics Anorectic Drugs | appetite suppressants or anorexiants | with treatments such as exercise. Prolonged use not recommended. Tolerance after several weeks. If tolerance to anorexigenic effect develops, discontinue drug |
| Mazindol (Mazanor) | Indirect Sympathomimetics Anorectic Drugs | appetite suppressants or anorexiants | with treatments such as exercise. Prolonged use not recommended. Tolerance after several weeks. If tolerance to anorexigenic effect develops, discontinue drug |
| Amphetamines; Dextroamphetamines; Methylphenidates | Indirect Sympathomimetics | Narcolepsy | |
| Modafinil (Schedule IV) Armodafinil (Schedule IV) | Indirect Sympathomimetics | Narcolepsy; shift work sleep disorder; obstructive sleep apnea/ hypopnea syndrome | Modafinil: Inhibit NE+DA uptake; increase amount of 5-HT & decrease GABA content with CNS nerve terminal (hypothalamus) Armodafinil (longer acting R-enantiomer) |
| Methamphetamine (Speed, Desoxyn) | Indirect Sympathomimetics drugs of Abuse | ADR: Xerostomia (dry mouth-stimulation alpha 2 POSTSYNAPTIC receptor); Isnomnia, seizures, excitability | |
| Cocaine | Indirect Sympathomimetics CNS stimulant | Local anesthetic topically for upper respiratory tract (oral, laryngeal, nasal mucous membranes) | Blocks reuptake of monoamines (NE, DA, 5-HT); HCL salt ADR: anxiety, agitation, tremor, delirium, hallucinations, paranoia, seizures CVS Effects: cardiac arrhythmias, acute hypertension, stroke, MI, hyperthermia |
| Pseudoephedrine | Mixed Acting Sympathomimetics | Nasal Decongestant | Increase NE release and weak agonist for alpha 1 and beta adrenergic receptors; alpha 1 effect constricts blood vessels in nasal mucosa |
| Ephedrine hydrochloride (REZIPRES); Ephedrine sulfate (EMERPHED) | Mixed Acting Sympathomimetics | Intraoperative hypotension caused by anesthesia | Increases NE release and weak agonist for alpha1 and beta adrenergic receptors |
| Metaraminol (ARAMINE) | Mixed Acting Sympathomimetics | Prevent hypotension during spinal anesthesia | Alpha1 adrenergic receptor agonist and increases NE release |
| Mephentermine (Wyamine Sulfate Injection) | Mixed Acting Sympathomimetics | Prevent hypotension during spinal anesthesia | Alpha1 adrenergic receptor agonist and increases NE release |
| All amphetamine-based products and Qelbree | Mixed Acting Sympathomimetics | Both direct (bind to 5-HT) and indirect |
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