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Drug Class Use Side Effects Interactions Other Very low acute toxicity “Schedule I” Δ9-tetrahydrocannabinol Anandamide Receptor Agonist “Many potential therapeutic uses” Lung cancer, CNS, Immunosuppression Testosterone suppression, Fetal damage “Little evidence for physiological dependence”

GAD & Panic OD & OSA Dose Dependent Effects-Not CNS Depressants Benzodiazepine Alcohol Alprazolam Anxiety with Depression ↑ Sedatives Require GABA to hyperpolarize; Lipophilic (GABA-A Receptors in CNS) dependency/withdrawal Panic Disorder Pregant, Elderly Hypnotics ↑ Potency, Higher dose for Panic than GAD

Antiviral Prevents viral uncoating, Prone to drug resistance Antiviral Amantadine (Influenza A) Anticholinergic effects Prevents infections of Influenza A Anti-Parkinson’s (Blocks DA reuptake into vessicles) Short term use in Parkinson’s

Stimulant Amphetamine ADD Similar to cocaine plus neurotoxicity (↓reuptake, ↑release of DA, 5HT, NE)

Benzocaine Ester Local Anesthetic Topical Minimal Lacks amine group - unionized

PNS & CNS Crosses BBB Benztropine Muscarinic Antagonist Parkinson’s Disease Treatment Can cause glaucoma crisis (↑ IOP) Good on tremor & rigidity, Bad on bradykinesia Not for Heart Disease or GI Obstruction

Partial D1 agonist; ergot alkaloid Peritoneal Fibrosis Bromocriptine D2 receptor agonist Parkinson’s Disease Treatment Adjunct to L-DOPA Similar to L-DOPA Less involuntary movement than L-DOPA

↑ CV Toxicity – Possibly V. Fib More potent & Longer duration than lidocaine Bupivacaine Amide Local Anesthetic Local, Regional & Epidural Proarrythmia – tachycardia Severe cardiotoxicity if given IV CNS Excitation then depression

Bupropion Depression Bupropion Contraindicated w/ psychosis (Wellbutrin) SSRI Sec Dysfunction (Wellbutrin)

No dependence/withdrawal Non-Benzodiazepine Buspirone Selective Anxiolytic Reduce dose for liver/kidney toxicity No cross tolerance w/ Benzo’s, no reaction w/ EtOH (5-HT1A Receptors in CNS) Very slow onset; good for elderly & subs abuse

Butorphanol Opioid Analgesic Asphyxia (kappa floor effect) Weak analgesic (kappa ceiling effect) (Stadol) (Selective kappa agonist) Tolerance & Physiological Dependence

Anxiety, Insomnia, Palpitations Caffeine A class all its own Makes medical education possible GI, HT, Dysrhythmias “#1 drug of social use” Corocary Thrombosis?

Iminostilbines Generalized Tonic-Clonic Lethargy, Ataxia, Diplopia Similar to TCAs, ↓ Absorption, Bound Carbamazepine (Binds Ca2+ & Na+ Channels) Partial Seizures Dose dependent neutropenia, ↓ Solubility, Metabolized to inactive compound (TCA-like – causes ↑ NE release) Bipolad Disorder Aplastic Anemia, Hyponatremia Variations in formulations (generics)

Decreases L-DOPA metabolism in periphery LAAD Inhibitor Carbidopa Parkinson’s Disease Treatment Increases CNS & motor effects of L-DOPA L-DOPA Doesn’t cross BBB; Reduces side effects? (Increase L-DOPA availability) Reduces required dose of L-DOPA by 75%

Chloroprocaine Ester Local Anesthetic Local & Regional CNS & CV Effects More potent but shorter duration than procaine Drug Class Use Side Effects Interactions Other Some Anti-Cholinergic,NE & Histamine effects Phenothiazine Sedative/Neuroleptic PD-like, Tardive dyskinesia (chronic), Chlorpromazine Offsets PD side effects slightly (DA receptor antagonist) (Anti-Psychotic/Schizophrenia) Amenorrhea, Photosensitivity, Dyscrasia Long t1/2, Renal Elimination

GAD & Panic OD & OSA Dose Dependent Effects-Not CNS Depressants Benzodiazepine Alcohol Clonazepam Panic Disorder dependency/withdrawal Sedatives Require GABA to hyperpolarize; Lipophilic (↑ Frequency of GABA-A Receptors) Absense Seizures Tolerance, Pregnant, Elderly Hypnotics Can ↓ spasms @ non-sedating dose

Anticholinergic/Sedation ↓D2, ↑5-HT & Ach receptor affinity Atypical Anti-psychotic Clozapine (Anti-Psychotic/Schizophrenia) Agranulocytosis, Blood Dyscrasia (5HT & ACh receptor antagonist) ↓ Extrapyramidal effects, Low Potency Orthostatic Hypotension Long t1/2, Renal Elimination, No Tardive Dyskinesia CNS ↑ & ↓, Vasoconstriction, Tachycardia, Stimulant/Anesthetic Local Anesthetic Amphetamine “ Cocaine Hyperthermia, HT, ↓RR, Dysrhythmia Probably the most rewarding drug” (Prevents re-uptake of DA & NE) (Opthalmology/ENT) Heroin Stroke, Paranoid Psychosis, Cardiotoxic Causes vasoconstriction

Abuse potential (Schedule II/III) Analgesic Codeine Opiate Analgesic Tolerance & Physiological Dependence NSAID ↑ Metabolized by CYP2D6 to morphine Cough Suppressant Overdose & Withdrawal

Halogenated Alkane Airway Irritation Very rapid onset & recovery, MAC = 6% Anesthesia (Inhaled) Desflurane Anesthetic Gas Dose dependent hypotension Dose dependent hypotension (Outpatient surgeries) (GABA Potentiation?) ↑ HR Little metabolism; Expensive

GAD & Panic (oral, IV, IM) Fatal OD Dose Dependent Effects-Not CNS Depressants Benzodiazepine Alcohol Diazepam Muscle Spasms, Status Epilepticus Obstructive Sleep Apnea (OSA) Sedatives Require GABA to hyperpolarize; Most Lipophilic (↑ Frequency of GABA-A Receptors) Hypnotics EtOH withdrawal, pre-op sedation Tolerance, Pregnant, Elderly Long t1/2

Disulfiram Aldehyde Dehydrogenase Antagonist Alcohol Dependece

COMT Inhibitor Increases L-DOPA available to brain Entacapone Parkinson’s Disease Treatment (Increase L-DOPA availability) Crosses BBB; Reduces side effects?

Diarrhea, Oxytocic (not for pregnant) Agonist or antagonist at 5HT, D2 & Adrenergic Migraine Headache Ergotamine Nonselective 5-HT Agonist ERgotism: cramps, paresthesia, angina If oral, given with caffeine to ↑ absorption (Nasal Spray > Oral) edema & ischemia; Causes dependency Given with metaclopramide for GI Upset

Non-Specific Risk taking, Lack of restraint, Violence Dose dependent effects; Blocks Gluconeogenesis Anxiolytic (GABA) Ethanol (GABA Receptor activation) Withdrawal Symtoms, ↓ REM Sleep 95% Metabolized in liver; Zero order elimination Amnestic/Anesthetic (Glu/NMDA) (Glu/NMDA Receptor Inhibition) GABAR change; ↑ # NMDAR Eliminated unchanged in urine, breath & sweat

??? Lipophilic but H2O Soluble, Not bound GI Ethosuximide Blocks t-Type Ca2+ Channels in Absence Complete GI absorption Headache Thalamaus Metabolized in liver (inactive), Long t1/2

Ultra short acting (5 minutes) ??? Anesthesia (IV) Muscle Spasms (Tx w/ diazepam) Etomidate Not for prolonged sedation of critically ill (Not a barbiturate) (Short Procedures) Dose dependent cortisol decrease Requires airway monitoring

Abuse potential (Schedule II) Opioid Analgesic Analgesic & Anesthetic Fentanyl Tolerance & Physiological Dependence ↓ (Selective mu agonist) (CV Surgery) RR can be reversed with naloxone Overdose & Withdrawal, ↓ RR, Pruritis

Benzodiazepine Overdose Flumazenil Benzodiazepine Antagonist (IV) Drug Class Use Side Effects Interactions Other ↓ P450 Most activating (insomnia) Fluoxetine SSRI Depression GI,CNS Activating, Sexual, ↑ Weight TCAs Biggest P450 Inhibitor, Worst GI (Prozac) (Block reuptake of 5HT) MAOIs Hypericum Least selective, Active metabolite, long t1/2

PD-like, Tardive dyskinesia (chronic), 3 Halogens = Most Potent Anti-psychotic Phenothiazine Sedative/Neuroleptic Fluphenazine Amenorrhea, Photosensitivity, Dyscrasia ↓ (DA receptor antagonist) (Anti-Psychotic/Schizophrenia) sedative, ↑extrapyramidal effects Neuroleptic malignant syndrome Long t1/2, Renal Elimination

OD & OSA Dose Dependent Effects-Not CNS Depressants Benzodiazepine Hypnotic Alcohol Flurazepam Daytime sedation Sedatives Require GABA to hyperpolarize; Lipophilic (↑ Frequency of GABA-A Receptors) (Inpatient – Long acting) Hypnotics Tolerance, Pregnant, Elderly Active Metabolite & Longest t1/2

Butyrophenone ↓ Sedative/Neuroleptic Acute PD-like sedative, ↑extrapyramidal effects Haloperidol Not A Phenothiazine! (Anti-Psychotic/Schizophrenia) Chronic = Tardive dyskinesia Acts on D2 receptors like phenothiazines (DA receptor antagonist) Long t1/2, Biliary Elimination

Halogenated Alkane Malignant Hyperthermia & Hepatitis High potency, low solubility, No analgesia < 1 MAC Halothane Anesthetic Gas Anesthesia (Inhaled) Arrythmias & ↑ Intracranial Pressure Catecholamines Some liver metabolism (no F- release)

(GABA Potentiation?) Hypotension & ↓ Respiration ↓ BP & CO, ↑RR? (↓ Respiration), ↓CO2 Response

Abuse potential (Schedule I) Heroin Opioid Analgesic Tolerance & Physiological Dependence Di-acetyl morphine Overdose & Withdrawal

Halogenated Alkane Slightly ↓ potency & ↓ solubility Anesthesia (Inhaled) Isoflurane Anesthetic Gas Dose dependent hypotension ↓ (DOC for neuroanesthesia) BP & CO, ↑ muscle relaxation; No ↑ ICP (GABA Potentiation?) No convulsive activity or hepatotoxicity

Dissociative Anesthetic Veterinary Medicine Confusion, “Schedule II?” Ketamine (Glu/NMDA receptor antagonist) Trauma & Emergency Surgeries Paranoia, Delusions & Hallucinations Marked analgesia & amnesia (Sigma receptor agonist) Cardiac Surgery & Ped Radiology Violence, Hyperthermia, Abuse Normal CO2 response, ↑ HR, CO & BP

Phenyltriazines Partial Seizures + Jacksonian Dizziness, Headache, Ataxia, Somnolence Phenytoin ↓ An adjunct, t =dependent on other medications Lamotrigine (Binds Ca2+ & Na+ Channels) Absence Seizures Carbamezapine ↓ 1/2 Rash (Metabolites-avoid by slow increase) 55% bound, slightly soluble (Inhibits Glu & Asp release) Neonatal (Lennox Gastaut) Valproic Acid ↑

Increase cell loss? 95% metabolized in periphery Dopamine Synthesis Activator L-Dopa Parkinson’s Disease Treatment Orthostatic HT & Dysrhythmias Crosses BBB; ↓ response after 2 years (Avoids rate limiting step in synthesis) GI, CNS, motor effects No effect on cognitive decline, efficacy fluctuates

Somnolence Soluble (Zwitterion at ph 7.4) Levetiracem ??? Partial Seizures + Jacksonian Dizziness Not metabolized, renal clearance (good for liver tox) (Keppra) Blocks N Type Ca2+ Channels(NMDA) Headache ↓ bound, t1/2 = 6 hrs

Anti-Arrythmic (Class IB) 2nd choice V. Tach suppression Proarrythmia – new ventricular tachycardia Minimal EKG effect & short DOA Lidocaine (weakly blocks Na+ Channel) Not for arrythmias Agitation Intermediate acting, Rapid hepatic metabolism Amide Local Anesthetic Local, Regional, Topical & Epidural CNS Excitation then depression Highly protein bound

Lithium Bipolar/Manic Depression Renal Elimination

GAD & Panic (oral, IV, IM) OD & OSA Dose Dependent Effects-Not CNS Depressants Benzodiazepine Alcohol Lorazepam Anxiety with Depression dependency/withdrawal Sedatives Require GABA to hyperpolarize; Lipophilic (↑ Frequency of GABA-A Receptors) Status Epilepticus Tolerance, Pregnant Hypnotics Conjugated=Not active

LSD-25 (Lysergic Acid Diethylamide) Drug Class Use Side Effects Interactions Other Abuse potential (Schedule II) Meperidine Opioid Analgesic Tolerance & Physiological Dependence Parkinson’s Disease associated w/ manufacture? (Demerol) (Moderate mu & kappa agonist) Overdose & Withdrawal

Tolerance & Physiological Dependence Methadone Opioid Analgesic Prevent Opiod Withdrawal Overdose & Withdrawal

Halogenated Alkane Very potent, ↑ solubility, analgesic at < MAC (.16%) Methoxyflurane Anesthetic Gas Anesthesia (Inhaled) Renal Toxicity (20% mortality) Catecholamines good muscle relaxant except uterus (GABA Potentiation?) ↑ Metabolism & ↑ F- release = renal toxicity

ADHD, Hypotension & Narcolepsy Methylphenidate Abuse & Tachyphylaxis Indirect Adrenergic Agonist Promotes Release/Inhibits Reuptake (Ritalin) Arrythmias, Hypertension & ↑ or ↓ HR (DA, NE, Serotonin)

5-HT Antagonist in periphery, Agonist in CNS Methysergide 5-HT Agonist/Antagonist Migraine Headache Fibrosis Don’t use for > 6 mos without 3-4 week “holiday” Only for not responsive to other prophylactics

Effetcts can be reversed with flumazenil Midazolam Benzodiazepine Pre-op Anesthesia & Amnesia (IV) Respiratory Arrest if pretreated w/ narcotic Alcohol Sedatives No analgesic effects (Versed) (↑ Frequency of GABA-A Receptors) Muscle Relaxant or COPD Hypnotics Ultra-short t1/2

Abuse potential (Schedule II) Opiate Analgesic Morphine Analgesic Tolerance & Physiological Dependence From Papaver somniferum poppy plant (Strong mu/partial kappa agonist) Overdose & Withdrawal

Opiod Overdose/Coma Naloxone Opiate Receptor Antagonist Precipitate Withdrawal Poor GI absorption (used to prevent IV use) Prevent Dependence Relapse

Alcohol Dependence Reduces rewarding effects of alcohol Naltrexone Opiate Receptor Antagonist Opiod Overdose/Coma Precipitate Withdrawal Strong at mu & kappa receptors Prevent Dependence Relapse Longer acting than Naloxone

Cancer, Bronchitis, Emphysema, Asthma Makes teenagers look Acutely causes nausea & vomiting Nicotine Cholinergic Arteriosclerosis, Atheroma, HT “ Smoking = “biggest health disaster of this century” cool & glamorous” Stroke, Thrombosis, ↓ fetal growth

↑ Anesthetic Gas MAC (>1.0); Good analgesic < MAC (endorphins) Nitrous Oxide Anesthesia Supplement (Inhaled) Diffusional Anoxia (GABA Potentiation?) Benign to CV & Respiratory, No muscle relaxation Often combined w/ other drugs (ex. Fentanyl)

Tricyclic Antidepressant Overdose Active metabolite of amitryptyline Nortriptyline (Block reuptake of 5HT & NE) Depression Moderate sedation, anti-cholinergic, Long t , Active Metabolite (Pamelor) 1/2 (Blocks Histamine Receptors) Orthostatic HT & Cardiac block, Seizures Mildest side effects

Dose Dependent Effects-Not CNS Depressants Benzodiazepine GAD & Panic OD & OSA Alcohol Oxazepam Sedatives Require GABA to hyperpolarize; Lipophilic (↑ Frequency of GABA-A Receptors) EtOH withdrawal Pregnant Hypnotics Conjugated=Not active Short t1/2

Abuse potential (Schedule II) Oxycodone Opioid Analgesic Tolerance & Physiological Dependence NSAID ↑ Metabolized by CYP2D6 to morphine (Percodan) (mu agonist) Overdose & Withdrawal

SSRI GI,CNS Activating, Sexual, ↑ Weight ↓ P450 Fewest GI effects, Most potent Paroxetine (Block reuptake of 5HT) Depression Mild anti-cholinergic effects & sedation TCAs Worst extrapyrimidal (tremor) & sex dysfunction (Paxil) MAOIs (Antihistamine) Worst withdrawal, Not for kids Hypericum Drug Holidays for sex dysfunction Drug Class Use Side Effects Interactions Other Abuse potential (Schedule IV) Opioid Analgesic Pentazocine Tolerance & Physiological Dependence (Partial mu agonist/kappa agonist) Overdose & Withdrawal

Amnesia, Confusion, Paranoia Phencyclidine Dissociative Anesthetic Veterinary Medicine Delusions & Hallucinations (PCP) (Glu/NMDA receptor antagonist) Violence, Hyperthermia, Abuse

Overdose Monoamine Oxidase Inhibitor Food w/ tyramine Treat hypertensive emergency with  -blockers Phenelzine Atypical Depression Tyramine causes catecholamine release (Block degradation of 5HT, NE & DA) Pseudoephedrine Short t Hypertensive Emergency 1/2

Impaired Cognitive Development Barbiturate Neonatal Seizures Phenobarbital Hyperactivity, Additive Effects Enhances its own metabolism (↑ time of open GABA-A Receptor) Status Epilepticus Drosiness, Sedation, Addictive Potential

Hydantoin Generalized Tonic-Clonic Crystallizes (IM), Gum Hypertrophy ↓ Plasma/ ↑ Lipid Soluble, ↑ Bound Phenytoin (Binds Ca2+ & Na+ Channels) Partial Seizures Macrocytosis, GI, Sedation, NT Defects Many ↑ GI Absorption, Liver Metabolism (Rate Limited) 2+ (Blocks Ca influx, IPSPs) Status Epilepticus Allergies, Ataxia, Face & Hair Changes t1/2 = ~day, Variations in formulations (generics)

Metabolized in plasma & liver by esterases Procaine Ester Local Anesthetic Local & Regional CNS & CV Effects Less potent & short acting, rapidly absorbed

Egg lecithing allergies & Painful ??? Anesthesia (IV) Rapidly acting Propofol Vasodilation & Hypotension (Not a barbiturate) (Regional anesthesia - infusion) ↓ Bacterial Contamination/Sepsis BP, RR, CO2 response & Intracranial Pressure

↓ Atypical Anti-psychotic Extrapyramidal effects Risperidone (Anti-Psychotic/Schizophrenia) (5HT & DA receptor antagonist) Long t1/2, Renal Elimination No agranulocytosis

GI, CNS, dry mouth MAO-B Inhibitor Selegiline Parkinson’s Disease Treatment Abuse Potential Metabolized to amphetamine (Selective inhibitor of DA metabolism) Insomnia & Psychosis

Depression ↓ P450 Sertraline Drug Holidays for sex dysfunction Selective Serotonin Reuptake Inhibitor (Neurovegetative = 2 weeks) GI,CNS Activating, Sexual, ↑ Weight TCAs (Zoloft) MAOIs Least P450 Inhibitor, Least Drug Interactions (Cognitive = 4 weeks) Hypericum

Halogenated Alkane Very rapid onset & recovery, Sevoflurane Airway Irritation Anesthetic Gas Anesthesia (Inhaled) Hepatic metabolism & F- release; ↓ renal toxicity Dose dependent hypotension (GABA Potentiation?) Less airway irritation & no tachycardia

Structurally similar to Serotonin Triptan Migraine Headache Coroncary Vasospasm Ergotamine Sumatriptan MAOI Faster onset than DHE, but higher recurrence (Selective 5-HT Agonist) (SubQ or Nasal Spray) (Not for CV Disease or HBP) SSRI

CNS & CV Effects 10X more potent than procaine, Tetracaine Ester Local Anesthetic Local & Regional (10X more toxic than Procaine) Slower onset, longer duration

Barbiturate Hyperalgesia Ultra short acting, redistributed to tissue from brain Thiopental Anesthesia Induction (IV) (↑ time of open GABA-A Receptor) Painful tissue necrosis Rapidly acting (seconds)

Reduced sedative & extrapyramidal side effects Phenothiazine Sedative/Neuroleptic PD-like, Tardive dyskinesia (chronic), Thioridazine Increased anticholinergic effects (DA receptor antagonist) (Anti-Psychotic/Schizophrenia) Amenorrhea, Photosensitivity, Dyscrasia Long t1/2, Renal Elimination Drug Class Use Side Effects Interactions Other

COMT Inhibitor Increases L-DOPA available to brain Tolcapone Parkinson’s Disease Treatment (Increase L-DOPA availability) Crosses BBB; Reduces side effects?

Sulfamate Monosaccharide Somnolence & Fatigue An adjunct, 2+ + Phenytoin ↓ Not metabolized, renal clearance (good for liver tox) Topiramate (Binds Ca & Na Channels) Partial Seizures + Jacksonian Impaired concentration/mental slowing Carbamezapine ↓ (Binds GABA-A / Blocks Glu) Renal Stones, Paresthesias, ↓ Appetite ↓ bound, t1/2 = ~20 hrs

↓ P450 SSRI Short t Trazodone Depression GI,CNS Activating, Sexual, ↑ Weight TCAs 1/2 (Block reuptake of 5HT) MAOIs Used as sedative/hypnotic in elderly Hypericum

OD & OSA, Rebound Insomnia & REM Dose Dependent Effects-Not CNS Depressants Benzodiazepine Hypnotic Alcohol Triazolam Tolerance , Amnesia & violence Sedatives Require GABA to hyperpolarize; Lipophilic (↑ Frequency of GABA-A Receptors) (Sleep onset) Hypnotics Worst dependency/withdrawal Highest Potency, Short t1/2

PNS & CNS Trihexyphenidyl Muscarinic Antagonist Parkinson’s Disease Treatment Can cause glaucoma crisis (↑ IOP) Not for Heart Disease or GI Obstruction

Branched Chain Fatty Acid Absence & Myoclonic Seizures ↑ Valproic Acid NT Defects, GI, Liver Necrosis GI Absorption, 90% Bound, Highly Soluble (Binds Ca2+ & Na+ Channels) Generalized Tonic-Clonic, Migraines ↑ Phenobarbitol (Valproate) Ataxia & Tremor t1/2 = ~10 hrs, Oxidation metabolism (↑ GABA concentrations) Reflex Epilepsy, Partial Seizures Renal elimination Quick onset, short t Zolpidem Non-Benzodiazepine 1/2 Selective Insomnia Dizziness, Headache, Confusion Alcohol ↓ (Ambien) (GABA-A Receptors in CNS) Anxiolytic, anti-convulsant, muscle relaxant effect Minimal rebound insomnia

Long Acting NMJ Block Safe with compromised renal or liver function Atracurium Nondepolarizing NMJ Antagonist Less – Spontaneous Hydrolysis Short Onset Hoffman/Plasma Esterase elimination

Mad, Hot, Blind, Dry, Red Muscarinic Antagonist AChE Inhibitor Antidote PNS & CNS Atropine Treat OD with physostigmine (Jimson weed) Inhibits M receptors in PNS/CNS Can cause glaucoma crisis (↑ IOP) Crosses BBB

Long acting (not metabolized by ChE) Bethanechol Muscarinic Agonist Increase Urinary & GI motility Some PNS activity (not heart) Possibly selective for M4

Few side-effects Duration of 24 hours Cyclopentolate Muscarinic Antagonist Produce mydriasis & cycloplegia Minimally absorbed after instillation Doesn’t Cross BBB

Not active orally, Excreted unchanged in urine Histamine Release, Hypotension D-Tubocurarine Nondepolarizing NMJ Antagonist Block NMJ (40 min duration) Causes Histamine Release (Blocks ganglia) ↓ MAC of inhalational anesthetics

Not given orally - metabolized

Dobutamine Adrenergic Agonist CHF & Shock No effect on DA1 receptors

+ = 1 & 2 agonist / - = 1 agonist

Long duration of action Echothiophate Irreversible ChE Inhibitor Long acting Glaucoma treatment Cataracts, CNS, PNS, SNS, NMJ effects May cause cataracts Crosses BBB

Curare poisoning Edrophonium Reversible ChE Inhibitor PNS, SNS, NMJ effects Doesn’t Cross BBB Diagnostic for M. Gravis Drug Class Use Side Effects Interactions Other

Ganglionic Antagonist Orthostatic Hypotension Excreted unchanged in urine Hexamethonium Rapidly Reduce Blood Pressure (Competitive Nicotinic Blocker) Side effects similar to atropine Doesn’t Cross BBB

Dry secretions for intubation Mainly PNS Glycopyrrolate Muscarinic Antagonist Doesn’t Cross BBB Inhibit PNS muscarinic receptors Can cause glaucoma crisis (↑ IOP)

Isoflurophate (Dfp) Irreversible ChE Inhibitor Prolonged Miosis CNS, PNS, SNS, NMJ effects Crosses BBB

Adrenergic Agonist Not given orally – metabolized Isoproterenol Bronchodilation ( Agonist only) Minimal effect on Blood Pressure

Poorly absorbed orally Myasthenia Gravis Neostigmine Reversible ChE Inhibitor PNS, SNS, NMJ effects Agonistic at nicotinic receptors Increase Urinary & GI motility Doesn’t Cross BBB

Longer DOA than Curare Less Histamine Release/Doesn’t block ganglia Pancuronium Nondepolarizing NMJ Antagonist Histamine Release, Tachycardia Blocks M2 Receptors 4X more potent than D-Tubocurarine

Parathion Irreversible ChE Inhibitor Insecticide CNS, PNS, SNS, NMJ effects Crosses BBB

Phenoxybenzamine Irreversible 1 &2 antagonist Pheochromocytomas

Nonselective  &  antagonist Phentolamine 1 2 Pheochromocytomas (Competitive)

Phenethylamine Phenylephrine Opthalmologic - Mydriasis (Direct 1 agonist)

Atropine Poisoning Physostigmine Reversible ChE Inhibitor CNS, PNS, SNS, NMJ effects Crosses BBB Decrease IOP (miosis)

Pilocarpine Glaucoma Emergency Muscarinic Agonist PNS activity, CNS effects, Sweating DOC for Immediate Lowering of IOP Sustained release for glaucoma

M1>M3>M2 M1 Selective Pirenzepine Peptic Ulcers No effect on heart or CNS ↓ Muscarinic Antagonist Gastric Secretion without ↑ HR Doesn’t Cross BBB

AChE Inhibitor Antidote Works by nucleophilic attack Pralidoxime (2-Pam) Organophosphate Antidote Reactivates ChE Must be used quickly

Hypertension Edema – need to take a diuretic Selective  antagonist Potential benefit for heart, lipids & prostate Prazosin 1 (Vasodilation without ↑ HR) ↑ (Competitive) risk of cardiac event ALLHAT study indicates heart risk ↑ HDL & ↓ LDL / ↓ BPH Postural Hypotenstion & Syncope Drug Class Use Side Effects Interactions Other Airway Disease Exacerbation  &  antagonist 1st Clinical Approved Beta Blocker Propranolol 1 2 ↑ Peripheral Vascular Disease (Nonselective Prototype) May ↑ Triglycerides & ↓ HDL Diabetic Hypoglycemia; ↓ CNS Fxn

Motion sickness PNS & CNS Scopolamine Muscarinic Antagonist Crosses BBB Pre-anesthetic/Sleep aid Can cause glaucoma crisis (↑ IOP)

Soman Irreversible ChE Inhibitor Nerve Gas CNS, PNS, SNS, NMJ effects Crosses BBB

Potentiated by AChE Inhibitor – not reversed Short Term NMJ Blocker ↑ + Succinylcholine Depolarizing NMJ Antagonist K , Muscle Pain Not metabolized by AchE No long term use Malignant Hyperthermia ↓ MAC of inhalational anesthetics

Ganglionic Antagonist Orthostatic Hypotension Trimethaphan Rapidly Reduce Blood Pressure Doesn’t Cross BBB (Competitive Nicotinic Blocker) Side effects similar to atropine

Duration of 6 hours Few side-effects Tropicamide Muscarinic Antagonist Produce mydriasis & cycloplegia Shortest t of any ophthalmologic drug Minimally absorbed after instillation ½ Doesn’t Cross BBB

Not an NSAID; Poorly inhibits COX Antipyretic & Analgesic Acetaminophen Central COX Inhibitor Hepatic Toxicicty (esp. with alcohol) No platelet function (Useful when aspirin contraindicated) No effect on acid/base or uric acid

Nausea, Vomiting, Diarrhea, BM Allergies Allopurinol Xanthine Oxidase Inhibitor Severe Gout & Renal Stones May induce Gout, BM Depression Probenecid Hepatic/Renal Toxicity, Cataracts

Integument Analgesic, Migraine Not for use with Peptic Ulcers; Reye’s COX Inhibitor (Covalently modifies COX1 & COX2) NSAID Aspirin Antipyretic, Antiinflammatory (↑ dose) Tinnitus, Deafness, Vertigo Suicide Inhibitor of COX1 & stimulator of LOX (Carboxylic Acid – Salicylate) Anticoagulant, Colon Cancer, MI Alkalosis,Acidosis,Fever, Dehydration Highly Dose Dependent – Not for Gout!

NSAID Rheumatoid Celecoxib (Selective COX2 Inhibitor) Reduced gastric toxicity Osteoarthritis (1st Gen)

Gout Diagnosic Diarrhea, Nausea, Vomiting, Hair Loss Relieves pain & inflammation of gout, not analgesic Plant Alkaloid Colchicine Gout (Inflammation Relief) Abdominal Pain, BM Suppression Inhibits tubulin polymerization/LTB4 (Neutrophils) (Autumn Crocus) Given <4 mg per week IV Peripheral Neuritis & Myopathy Greater than 8 mg is lethal

Antiinflammatory, Migraine NSAID Better tolerated than aspirin Ibuprofen Analgesic, Antipyretic (Propionic Acid) Also for Ankylosing Spondylitis & Dysmenorrhea Rheumatoid Arthritis & Osteoarthritis

NSAID Anti-inflammatory Inhibits prostaglandin inflammation of Gout Indomethacin Toxic (Acetic Acid) Gout Inhibits macrophage urate phagocytosis

Analgesic Poor inhibitor of inflammation NSAID Ketorolac Allergic Conjunctivitis Approved for topical, parenteral & oral use (Fenamic Acid) Occular Inflammation Short Term Use only

Severe! Cytoprotective to GI Tract, ↑ Blood Flow Misoprostol Prostaglandin Diarrhea & Uterine Contractions ↑ Mucus & Bicarb secretion Avoid in pregnancy ↓ cAMP in Parietal cell Drug Class Use Side Effects Interactions Other

N-Acetylcysteine Acetominophen Toxicity Precursor of glutathione

Not for use with kidney stones Not effective during acute attack Uricosuric Salicilate Probenecid Gout Increases gout Designed to inhibit penicillin excretion (Increases Uric Acid Excretion) Allopurinol Use with caution if peptic ulcers Additive with Sulfinpyrazone

NSAID Antiinflammatory Increased risk of CV thrombosis Inhibits the inducible COX-2 Rofecoxib (Selective COX2 Inhibitor) Rheumatoid Arthritis Renal Toxicity Longer t & smaller dose than Celecoxib (but qid) (1st Gen) Osteoarthritis & Acute Pain 1/2

Low doses ↑ urate reabsorption Uricosuric Like Probenecid – inhibits urate reabsorption Sulfinpyrazone Gout Gastric Distress & Peptic Ulcers Salicilates (Increases Uric Acid Excretion) Must use a loading dose ↑ Acetominophen toxicity, ↓ Hematopoiesis

Stimulate NTS to ↓ BP Α-Methyldopa Prodrug of Methylnorepinephrine Hemolytic Anemia (Decrease Sympathetics)

Blocks AV node by hyperpolarization Quickly stop supra-v tach Flushing & Brief cardiac arrest Theophylline ↓ Adenosine Anti-Arrythmic Short DOA (t of 6 seconds) Stops AV nodal reentry Bronchoconstriction Dipyridimole ↑ 1/2 Works on A1 receptor similar to M2

Arrythmias Lung toxicity ↑ Warfarin Prolonged QT interval Class III Anti-Arrythmic Amiodarone Immediate or long-term suppression (dyspnea, cough & pneumonitis) ↑ Digoxin Metabolized very slowly (t of weeks) (blocks K+ Channel) 1/2 DOC for stopping a. fib & v. tach Thyrotoxicosis or Hypothyroidism Especially useful if ↑ risk of proarrythmias

Angina (not unstable) Calcium Channel Antagonist Reflex Tachycardia, Edema & headache Amlodipine Hypertension Vasodilators Strong vascular effect (Dihydropyridine Class) Gingival hyperplasia (DOC for var. Angina prophylaxis)

↑ Phosphodiesterase Inhibitor Arrythmias & Thrombocytopenia Cardiac force & output; vasodilation & ↓ TPR Amrinone (Inamrinone) CHF (short term use) (↑ cAMP) Nausea & Vomiting No tolerance Not effective at ↓ morbidity & mortality of CHF

Hypertension, Cardiac Ischemia Atenolol Selective 1 antagonist Arrythmias, Anxiety ↓ CNS Fxn May ↑ Triglycerides & ↓ HDL (↓ HR & Force; ↓ Renin release)

↓ cholesterol synthesis, ↑ LDL receptors HMG-CoA Reductase Inhibitor Avoid in pregnancy & liver disease Atorvastatin Hyperlipidemia ↑ (Statin) ↑ Myopathy & Liver Transaminases HDL, ↓ LDL & TGs, antioxidant Extensive 1st pass hepatic metabolism (P450) Persistant cough ACE Inhibitor Hypertension & CHF Beneficial effect on serum lipids Captopril Can ↓ GFR in renal artery stenosis (Decrease TPR & hypertrophy) (1st Line) ↓ Angioedema Angiotensin II and Aldosterone

CHF & Hypertension

Carvedilol 1 & 2 antagonist (↓ Heart Dimensions) ↓ CNS Fxn May ↑ Triglycerides & ↓ HDL (Antioxidant & Antiproliferative)

Few – safe for pregnancy Bind anionic compounds (bile acids) Bile Acid Sequestrant Cholestyramine Hyperlipidemia May ↑ TGs ↑ (Resin) LDL receptors, ↓LDL GI disturbances not absorbed or metabolized

Stimulate NTS to ↓ BP Also for: drug withdrawal, headaches, diarrhea, Clonidine Direct  agonist Drowsiness, Dry Mouth 2 (Decrease Sympathetics) glaucoma, colitis, ulcerative colitis, Tourette’s Drug Class Use Side Effects Interactions Other Few – safe for pregnancy Bind anionic compounds (bile acids) Bile Acid Sequestrant Colesevelam Hyperlipidemia May ↑ TGs ↑ (Resin) LDL receptors, ↓LDL GI disturbances not absorbed or metabolized

Toxic (worse w/ age, ↓ K, hypoxia) Cholestyramine ↓ Inhibit heart Na+ K+ ATPase → ↑ Ca2+ 1) Cardiac Glycosides Amiodarone ↑ Digitoxin CHF & Supraventricular Tachycardia Nausea, CNS, arrythmias Verapamil ↑ ↓ SA,AV node conduction speed (AV = major) 2) Anti-Arrythmic + Treat w/ phenytoin, lidocaine, Fab, K Quinidine ↑ liver metabolism, ↑ absorption, ↑ t1/2

Toxic (worse w/ age, ↓ K, hypoxia) Cholestyramine ↓ Inhibit heart Na+ K+ ATPase → ↑ Ca2+ Amiodarone ↑ Digoxin Cardiac Glycosides CHF & Supraventricular Tachycardia Nausea, CNS, arrythmias Verapamil ↑ ↓ SA,AV node conduction speed (AV = major) + Treat w/ phenytoin, lidocaine, Fab, K Quinidine ↑ renal metabolism, ↓ absorption, ↓ t1/2

Angina (not unstable) 1) Calcium Channel Antagonist Bradycardia, AV block, hypotension Diltiazem Hypertension & Arrythmias  blockers Intermediate effect 2) Class IV Anti-Arrythmic (best tolerated) Digoxin (DOC for var. Angina prophylaxis)

Not given orally - metabolized

Dobutamine Adrenergic Agonist CHF & Shock No effect on DA1 receptors

+ = 1 & 2 agonist / - = 1 agonist

Persistant cough Enalapril ACE Inhibitor Hypertension & CHF Beneficial effect on serum lipids Can ↓ GFR in renal artery stenosis (Enalaprilat) (Decrease TPR & hypertrophy) (1st Line) ↓ Angioedema Angiotensin II and Aldosterone

Localizes to intestinal brush border Ezetimibe Cholesterol Absorption Inhibitor Hyperlipidemia Hypersensitivity Doesn’t disturb vitamin A,D,E absorption Often combined with statins

Anti-Arrythmic Significantly widens QRS Arrythmias Proarrythmia – new ventricular tachycardia Flecainide (Class IC) Should be avoided in structural heart disease DOC for A. Fib prevention Weakens cardiac contraction (strongly blocks Na+ Channel) Should be avoided in ↓ ventricular function

↑ Anticoagulants Ototoxic/hypotension/arrythmias ↑Lithium Diuretics Edema, CHF, Hypertension Furosemide ↑ Uric acid, LDL & TGs & glucose ↑ Propranolol Block Na+,K+,Cl- symporter in ascending loop Loop (High Celiling) Ascites, Hypercalcemia ↑ + 2+ + - 2+ Antiarrythmals ↓ K , Ca , Na , Cl & Mg Probenecid ↓ NSAIDS ↓ ↑ Ligand for nuclear PPARa receptor Hyperlipidemia non-CHD mortality, avoid in liver & Gemfibrozil Fibrate ↑ Bile Acid, Lipoprotein Lipase & HDL Acute Pancreatitis kidney disease; dyspepsia, myopathy, gallstones & GI complaints ↓ VLDL, Apo C, FAs (metabolized)

Adrenergic Neuron Blocker Hypertension Guanethidine Hypotension & Bradycardia No CNS interference (Sympatholytic) Inhibit NE release

Arterial Selective Vasodilator Lupus-like symptoms Hydralazine (Decrease TPR) Hypertension & CHF Headache, Tachycardia (↑ smooth muscle cGMP) Water and salt retention

↑ Uric acid & Ca2+ / ↓ K+ & Mg2+ ↓ Anticoagulants Block Na+,Cl- symporter in distal tubule Diuretic Hypertension & Edema ↓ Uricosorics Hydrochlorthiazide ↑ (some CA inhibition) Thiazide (↓ Peripheral Vascular Resistance) LDL & TGs / ↓ Glucose tolerance ↑ Antiarrythmals Impotence & Ventricular arrythmias NSAIDS ↓ Secreted by proximal tubule cells ↑ Inamrinone Phosphodiesterase Inhibitor Arrythmias & Thrombocytopenia Cardiac force & output; vasodilation & ↓ TPR CHF (short term use) (Amrinone) (↑ cAMP) Nausea & Vomiting No tolerance Not effective at ↓ morbidity & mortality of CHF

Adrenergic Agonist Not given orally – metabolized Isoproterenol Bronchodilation ( Agonist only) Minimal effect on Blood Pressure Drug Class Use Side Effects Interactions Other Vasodilation (esp. of large veins); stop vasospasm Organic Nitrate Myocardial Ischemia Excessive vasodilation Isosorbide Dinitrate Sildenafil ↑ Converted to NO in mitochondria; (↑ smooth muscle cGMP) (DOC for angina termination) Heaches, Hypotension & Tachycardia Slow onset but better bioavailability & DOA

Orthostatic Hypotension, ↓ CNS Fxn Labetalol Hypertension 1 & 2 antagonist Fatigue

Anti-Arrythmic (Class IB) 2nd choice V. Tach suppression Proarrythmia – new ventricular tachycardia Minimal EKG effect & short DOA Lidocaine (weakly blocks Na+ Channel) Not for arrythmias Agitation Intermediate acting, Rapid hepatic metabolism Amide Local Anesthetic Local, Regional, Topical & Epidural CNS Excitation then depression Highly protein bound

Angiotensin II Antagonist Hypertension & CHF Bind AT1 receptor reversibly Losartan (Decrease TPR & hypertrophy) (1st Line) (EXP 3174 has higher affinity)

CHF & Hypertension Metoprolol Selective 1 antagonist ↓ May ↑ Triglycerides & ↓ HDL Myocardial Ischemia CNS Fxn

Less toxic than amrinone ↑ Phosphodiesterase Inhibitor Cardiac force & output; vasodilation & ↓ TPR Milrinone Arrythmias & Thrombocytopenia (↑ cAMP → ↑ force & output) No tolerance Nausea & Vomiting Not effective at ↓ morbidity & mortality of CHF

Hypertension Stimulates K+ channel to hyperpolarize cell Minoxidil Arterial Vasodilator Typical arterial vasodilator effects (Hair Growth) Reserved for more severe hypertension

Hepatotoxic (less in crystalline form) Effective at ↑ levels above normal vitamins Nicotinic Acid (Niacin) Vitamin Hyperlipidemia Flushing, Hyperglycemia, Gout Decreases FA mobilization, renal excretion

Upper GI distress ↓ LDL & TGs, ↑ HDL; short t1/2

Angina (not unstable) Calcium Channel Antagonist Reflex Tachycardia, Edema & headache Nifedipine Hypertension Vasodilators Strong vascular effect (Dihydropyridine Class) Gingival hyperplasia (DOC for var. Angina prophylaxis)

Vasodilation (esp. of large veins); stop vasospasm Organic Nitrate Myocardial Ischemia Tolerance & Excessive vasodilation Nitroglycerin Sildenafil ↑ Converted to NO (mitochondria); volatile (↑ smooth muscle cGMP) (DOC for angina termination) Heaches, Hypotension & Tachycardia Rapid onset but short DOA & ↓ bioavailability

Arterial & Veinous Vasodilator Hypertensive Emergencies Hypotension Unstable in solution & Light Sensitive Sodium Nitroprusside (↑ smooth muscle cGMP) Acute CHF Cyanide & Thiocyanate metabolites Short DOA

Hypertension Edema – need to take a diuretic Selective  antagonist Potential benefit for heart, lipids & prostate Prazosin 1 (Vasodilation without ↑ HR) ↑ (Competitive) risk of cardiac event ALLHAT study indicates heart risk ↑ HDL & ↓ LDL / ↓ BPH Postural Hypotenstion & Syncope

Weaker contractions Anti-Arrythmic (Class IA) Procainamide Arrythmias Torsade de Pointes (EAD arrythmias) K+ blockers Widens QRS (Na+) & Prolongs QT ( K+) (blocks Na+/ K+channel) Lupus-like syndrome & BM depression

Adrenergic Neuron Blocker Hypertension Reserpine Insomnia, Sedation & Depression (Sympatholytic) Destroy NE storage granules

↓ cholesterol synthesis, ↑ LDL receptors HMG-CoA Reductase Inhibitor Avoid in pregnancy & liver disease Simvastatin Hyperlipidemia ↑ (Statin) ↑ Myopathy & Liver Transaminases HDL, ↓ LDL & TGs, antioxidant Extensive 1st pass hepatic metabolism (P450) Drug Class Use Side Effects Interactions Other Anti-Arrythmic Arrythmias Torsade de Pointes Sotalol Class II & III Anti-Arrythmic Avoid with CHF & structural disease + DOC for A. Fib prevention Asthma & bronchoconstriction 1 & 2 and K Channel blocker Low doses ↑ urate reabsorption Uricosuric Like Probenecid – inhibits urate reabsorption Sulfinpyrazone Gout Gastric Distress & Peptic Ulcers Salicilates (Increases Uric Acid Excretion) Must use a loading dose ↑ Acetominophen toxicity, ↓ Hematopoiesis

Angina, Hypertension, Arrythmias 1) Calcium Channel Antagonist Verapamil (DOC for var. Angina prophylaxis) Bradycardia, AV block, hypotension  blockers strong cardiac effect 2) Class IV Anti-Arrythmic Digoxin (DOC for A. Fib rate control)

Allergies, GI Upset -Lactam Oral Amoxicillin Superinfections Prophylactically by dentists (Penicillin) URI, Sinusitis, Otitis & LRTI (DOC) (Aminopenicillin) Non-allergic skin rashes

Allergies, GI Upset -Lactam Anaerobes, enterococci, Listeria Ampicillin Parenteral (IV) Superinfections (Penicillin) Gram- rods & bacilli, (E. coli, H. inf, Salmonella) (Aminopenicillin) Non-allergic skin rashes

Similar to above; pnce/day dose; well tolerated Protein Synthesis Inhibitor Azithromycin Legionella (DOC) Ototoxicity Less GI upset, Few interactions Macrolides Doesn’t inhibit P450

Allergies Surgical Prophylaxis Cefazolin -Lactam Parenteral (1st Generation Cephalosporin) Potentially nephrotoxic Bone Penetration

Allergies Ceftazidime -Lactam Parenteral Pseudomonas (3rd Generation Cephalosporin) Potentially nephrotoxic

Gets in CSF Parenteral Allergies Ceftriaxone -Lactam Great for N. gonrrorhea; Longest t rd Meningitis & Lyme Disease (DOC) Potentially nephrotoxic 1/2 (3 Generation Cephalosporin) Excreted in bile (not renal); Penetrates bone

Allergies Cephalexin -Lactam Oral (1st Generation Cephalosporin) Potentially nephrotoxic

Macrolides Oral & Parenteral Gray Baby Syndrome, GI Upset Binds 50S, prevents bond formation Protein Synthesis Inhibitor Clindamycin Chloramphenicol Bacteristatic ↓ Anticoagulants Broad Spectrum, Gets in CSF Chloramphenicol Clotting (↓ Vitamin K), Allergies S. typhi, Abscesses, Mixed Infections Anti-HIV meds Hepatic Metabolism (glucuronate), renal secretion BM Depression, Black Tongue Phenytoin ↑ Theophylline Nucleic Acid Synthesis Inhibitor Nausea, Headache, Dizziness Gram -, UTI, Prostatitis, Pseudomonas in CF UTI (DOC) ↑ Warfarin Ciprofloxacin (Fluoroquinolones & Quinolones) Nephrotoxic & Phototoxic Synergystic with  -Lactams Anti-TB (2nd line) ↑ Cyclosporine Not for pregnant or under 18, Seizures NSAID ↑ Antacids ↓ ↑ Warfarin Improved acid stability, same as above & Toxoplasma, Protein Synthesis Inhibitor ↑ Steroids Clarithromycin Ototoxicity ↑ M. leprae & avium, longer t Macrolides Digoxin 1/2 ↑ Carbamexzapime Less GI upset, renal elimination, Inhibits P450 Others

Clavulanic Acid overcomes  -Lactamases

Oral (well absorbed) & Parenteral Binds 50S, prevents translocation Clindamycin Diarrhea, Colitis, ↓ hematopoietic Chloramphenicol Clindamycin Bactericidal Gram + & - , anaerobes; Gets in bone (Cleocin) Inhibits NMJ Macrolides Anaerobic Infections (DOC) Metabolized in liver, excreted in bile Drug Class Use Side Effects Interactions Other Parenteral (slow IV) Binds two sites on 50S, prevents translocation Dalfopristin Protein Synthesis Inhibitor Pain & Phlebitis at infusion site ↑ Calcium Blockers Bacteristatic (some cidal) Gram +, Few Gram – (Moraxella & Neiserria) (Synercid) Streptogramin Arthalgias & Myalgias ↑ Cyclosporine Reserved for resistant Gram + Hepatic elimination (conjugation)

Protein Synthesis Inhibitor Bones & Teeth, Hepatotoxic, GI upset Antacids ↓ Doxycycline Oral ↓ Birth Control Liver metabolism, Hepatic excretion Tetracycline Not for pregnant or children, Phototoxic ↑ Anticoagulants

↑ Warfarin Oral GI Upset (direct stimulation) Destroyed by gastric acid (coated), Protein Synthesis Inhibitor ↑ Steroids Erythromycin Parenteral (IV) Ototoxicity, not for hepatic disfxn pts ↑ Hepatic elimination; Penicillin alternative Macrolides Digoxin Chlamydia UG infections (DOC ↑ Carbamexzapime Inhibits P450 Others Ototoxicity (worst of all aminoglycosides) Endocarditis (+  -Lactam); Severe UTI Protein Synthesis Inhibitor Gentamicin Parenteral Nephrotoxicity, vestibular damage Pseudomonas, Klebsiella, Proteus, Serratia, brucellosis, Aminoglycoside Neuromuscular paralysis (w/ ↑ doses) tularemia, peritonitis; Binds 30 & 50S

GI Upset, rash Gram + & - & Anaerobes DOC = enterobacter Parenteral (IV) Imipenem-Cilastatin Carbapenem Reaction at infusion site Gets in bones & CSF, Renal Clearance Reserved Seizures with renal insufficiency Given with Cilastin to prevent inactivation

Oral Prevents formation of f-met tRNA w/ 70S Protein Synthesis Inhibitor Thrombocytopenia, GI Upset, Headache Linezolid Bacteristatic (some cidal) Gram +; non-enzymatic oxidation Linezolid Rash Reserved for resistant Gram + Renal Elimination

-Lactam Allergies Methicillin Parenteral (IV) (Penicillin) Nephrotoxic -Lactamase producing Staph (Antistaphylococcal)

Oral Nausea, Headache, Vertigo Fragments anaerobic DNA, must be reduced Metronidazole Nucleic Acid Synthesis Inhibitor Bactericidal Alcohol Intolerance Gets into bone & CSF Bacteroides (DOC) Peripheral Neuropathy Liver & Renal Metabolism/Excretion; Enterocolitis

-Lactam Allergies -Lactamase producing Staph Nafcillin (Penicillin) Parenteral (IV) Nephrotoxic Preferred over methicillin (Antistaphylococcal)

Parenteral (IV & IM) Allergies IV DOC = strep,meningcocci, enterococci, Penicillin G -Lactam Syphilis (DOC – given IM) Seizures (w/ ↑ dose in renal failure) pneumococci, bacillus & clostridium (Penicillin V) (Penicillin) (Standard Penicillin) Oral(V) Allergies (V) Some anaerobes, minor infections (V)

-Lactam Gram – (Klebsiella, Enterobacter, Pseudomonas) Piperacillin (Penicillin) Allergies Often combined with aminoglycoside (tobramycin) (Antipseudomonal) For hospitalized neutropenic patients

Parenteral (slow IV) Binds two sites on 50S, prevents translocation Quinupristo Protein Synthesis Inhibitor Pain & Phlebitis at infusion site ↑ Calcium Blockers Bacteristatic (some cidal) Gram +, Few Gram – (Moraxella & Neiserria) (Synercid) Streptogramin Arthalgias & Myalgias ↑ Cyclosporine Reserved for resistant Gram + Hepatic elimination (conjugation)

2nd line TB, plaque, Tularemia (+penicillin) Protein Synthesis Inhibitor Parenteral Vestibular damage/fetal hearing loss Streptomycin Resistance is a problem; Doesn’t cross BBB Aminoglycoside Anti-TB Neuromuscular paralysis (w/ ↑ doses) Binds 30S, not metaboolized

Nephrotoxicity (crystalluria), Allergies Methenamine UTI, Otitis, Bronchitis, Sinusitis, PCC Pneumonia Metabolic Inhibitor Oral ↑ Anticoagulants Sulfamethoxazole Not for pregnant & newborns (kernicterus) Trachoma, Nocardiosis (Sulfonamide) Suppository ↑ Anticonvulsants Anemia (G6PD) ↑ Hypoglycemics Often combined with Trimethoprim

(Co-Trimoxazole) Drug Class Use Side Effects Interactions Other

Antacids ↓ Liver metabolism,renal excretion Protein Synthesis Inhibitor Bones & Teeth, Hepatotoxic, GI upset Tetracycline Oral ↓ Birth Control DOC = Rickettsias, cholera, Borrelia, Tetracycline Not for pregnant or children, Phototoxic ↑ Anticoagulants Chlamydia, Mycoplasma, Brucella, Tularemia, Acne

Ototoxicity, nephrotoxicity Similar to gentamycin, better w/ Pseudomonas Protein Synthesis Inhibitor Tobramycin Parenteral vestibular damage Less w/ Serratia & enterococci Aminoglycoside Neuromuscular paralysis (w/ ↑ doses) Oftened combined with  -Lactam; Binds 30 & 50S

Same as sulfa Binds DHF reductase ;Concentrates in prostate & vaginal Trimethoprim Metabolic Inhibitor Oral Bad for AIDS w/ PCCP (Stevens-Johnson) fluids; UTI, prostatitis, genital infxns, Legionella, Permanent renal damage if ↓ function Salmonella, “anythingitis” & PCCP Red Man Syndrome Parenteral (Slow IV) Prevents formation of polymers in cell wall Fever, Chills, Phlebitis, Tachycardia Vancomycin Vancomycin Oral (for colitis) Aminoglycosides Gram +, MRSA, Clostridium, Enterococci Hypotension, Shock, Flushing Reserved Renal secretion, Penetrates CSF with inflammation Allergies, Ototoxic, Nephrotoxic Inhibits viral DNA synthesis, chain elongation Antiviral Antiviral Acyclovir Renal clearance, requires Thymidine Kinase (Herpes) Oral or Parenteral (IV) Guanosine analog, binds viral DNA Polymerase

Antiviral Prevents viral uncoating, Prone to drug resistance Antiviral Amantidine (Influenza A) Anticholinergic effects Prevents infections of Influenza A Anti-Parkinson’s (Blocks DA reuptake into vessicles) Short term use in Parkinson’s

Fever, Chills, Allergic Reaction Polyene Macrolide Systemic Administration Binds ergosterol, Significant Renal Toxicity Amphotericin B Renal Dysfunction, Hypotension, Fungal Membrane Disruption (Broad Spectrum Antifungal) Not for oral use Hypokalemia, Anemia, Thrombophlebitis

ddI Antiviral (ddInosine) Reverse Transcriptase Inhibitor

Antiviral Didanosine Reverse Transcriptase Inhibitor

Optic Neuritis (blurring, loss of green) CSF Distribution less than serum; Not metabolized Ethambutol Tuberculocidal Oral Anaphylaxis, Dermatitis, Anorexia Must be monitered for visual acuity since optic neuritis is Nausea reversible Warfarin Triazole DOC = Candidosis Altered drug metabolism/sterol synthesis Cyclosporine Slower metabolism; Less effect on human sterols Fluconazole Sterol Synthesis Inhibitor DOC = Cryptococcal Meningitis Teratogen Phenytoin Crosses BBB (Lanosterol Demethylase Inhibitor) DOC = Coccidiodal Meningitis Nausea, Vomiting, Rash Lovastatin Inhibits P450 Protease Inhibitors Pyrimidine Requires cytosine specific permease, Crosses BBB BM Depression Flucytosine DNA & Protein Synthesis Inhibitor Oral Antifungal Converted to 5-FU; Resistance via ↓ uptake Nausea, Vomiting, Diarrhea (Thymidilate Synthase Inhibitor) Synergistic with Amphotericin B

Oral Antifungal Drug Interactions Fungal Mitosis Inhibitor Specific to fungi; Concentrates in skin Griseofulvin (Microsporum, Trichophyton & Allergic Reactions, Headache, Nausea (Binds Microtubules) Induces P450 Epidermophyton) Liver Toxicity?

Peripheral Neuritis (Vitamin B6) Tuberculocidal Isoniazid Oral Rash, fever, hepatotoxic Crosses BBB/CSF; Metabolized by N-acetyl transferase (Mycolic Acid Synthesis Inhibitor) Hypersensitivity

Imidazole Altered drug metabolism/sterol synthesis TInea corporis, Tinea pedis, Miconazole Sterol Synthesis Inhibitor Teratogen Topical use only Vaginal Candidosis (Lanosterol Demethylase Inhibitor) Burning, Itching, Irritation Drug Class Use Side Effects Interactions Other

Antiviral Nevirapine Blocks active site of reverse transcriptase Non-nucleoside RTI

Oral Candidosis Polyene Macrolide Bitter Taste Nystatin Topical Administration Highly toxic if given IV Fungal Membrane Disruption Minimal Oral Absorption (Broad Spectrum Antifungal)

Bacteriostatic Tuberculocidal Hepatitis Pyrazinamide Oral Resembles Nicotinamide; Crosses BBB (Mycolic Acid Synthesis Inhibitor?) Hyperuricemia Metabolized in liver; renal excretion

Oral Makes body fluids red ↓ Anticoagulants Inhibits RNA Pol; Deacetylation for activation ↓ Rifampin Nucleic Acid Synthesis Inhibitor Bactericidal Hepatotoxic Contraceptives Gram + & -, Mycobacteria, N. meningitides ↓ Glucocorticoids Anti-TB GI Upset, bleeding, flu-like ↓ Estrogen Hepatic metabolism, enterohepatic recirculation

Rifamycin Similar to Rifampin Rifapentine Similar to Rifampin Similar to Rifampin Easier dosing than Rifampin (once weekly)

Prevents viral uncoating Antiviral Antiviral Rimantidine Anticholinergic effects Prevents infections of Influenza A (Influenza A) Anti-Parkinson’s Prone to drug resistance

Antiviral Inhibit cleavage of pol & gag proteins by protease Saquinavir Protease Inhibitor Progeny virions lack ability to reproduce

Allyamine Tinea Infections Allergic reactions if given orally Oral, Topical, Future use Systemically? Terbinafine Sterol Synthesis Inhibitor Nail Infections Not for use if hepatic impairment Concentrates in skin and nails (Squalene Epoxidase Inhibitor) Bronchial Aspergillosis? Dose adjustment for renal impairment

Antiviral Antiviral Preffered over acyclovir for genital herpes & VZV Valcyclovir (Herpes) Oral Valine ester of acyclovir, better absorption

Antiviral Antiviral Pyrimidine analog, targets reverse transcriptase Zidovudine (AZT) Reverse Transcriptase Inhibitor Oral Gets in CSF, renal elimination

Diarrhea, constipation, renal problems Aluminum Hydroxide Antacid GERD & PUD ↑ Diazepam Neutralize gastric acid Altered drug absorption

Severe intestinal cramping Stimulates nerve plexus of colon Constipation Bisacodyl Diphenylmethane Derivative Low Grade Inflammation Given orally (slow) or rectally (fast), Pre-op colonic cleanse Permanent constipation hydrolyzed in stomach; excreted in stool

Bismuth GERD & PUD Sooths, Coats, Protects gastric mucosa

Antihistamine Mental confusion, Renal Disturbances Lidocaine Prevents nocturnal acid; Given orally or IV Cimetidine GERD & PUD (Reversible H2 Antagonist) Liver function abnormalities Diazepam Rapidly absorbed; Inhibits P450 metabolism

Binds  opioid, Shorter onset than Loperamide CNS effects at ↑ doses Diphenoxylate Opioid Diarrhea Combined with atropine to discourage abuse Abuse potential t1/2 = 12 hours Drug Class Use Side Effects Interactions Other Fecal softener, lower surface tension of stool Ducosates Stool-wetting agent Constipation Reduce strain of defacation Little proven efficacy

Entanercept TNF- Antagonist Crohn’s Disease TNF- Receptor coupled to Fc portion of IgG1

Anti-nausea/Anti-emetic Nausea & Vomiting Constipation, Diarrhea, Headache, Oral or IV; prolonged interaction; P450 metabolism Granisetron (5-HT3 Antagonist) (Chemotherapy induced) Lightheadedness

Lupus? Infliximab TNF- Antagonist Crohn’s Disease Chimeric Immunoglobulin; 2/3 patient response Lymphoma?

Emetic Quickly induces vomiting Ipecac Poisoning Use Carefully (plant alkaloids) Acts on CTZ & irritates stomach & duodenum

Binds  opioid; Poor CNS penetration CNS effects with overdose Loperamide Opioid Diarrhea Inhibits secretion of cholera,E. Coli toxins Children more sensitive than adults Liver metabolism, t1/2 = 11 hours

Neutralize gastric acid Mg(Oh)2/Co3 Antacid GERD & PUD Diarrhea, constipation, renal problems ↓ Diazepam Poorly absorbed, draws H2O into intestine (Milk Of Magnesia) Osmotic Agent Constipation Altered drug absorption Increases peristalsis

BM Loss Inhibits lymphocyte proliferation 6-mercaptopurine Immunosuppresive Infection Takes 3-6 months to work Teratogenic

Parkinson’s like symptoms GERD (rarely used) Agonist to 5-HT , antagonist to 5-HT & D Metoclopramide Prokinetic Extrapyramidal effects, restlessness, 4 3 2 Promotes gastric emptying, suppresses vomiting Sedation, diarrhea, nausea, fatigue

Fecal softener, lower surface tension of stool Mineral Oil Stool-wetting agent Constipation Reduce strain of defacation Little proven efficacy

Severe! Cytoprotective to GI Tract, ↑ Blood Flow Misoprostol Prostaglandin Diarrhea & Uterine Contractions ↑ Mucus & Bicarb secretion Avoid in pregnancy ↓ cAMP in Parietal cell Hypochlorhydria, Bacterial overgrowth Benzodiazepines Accumulates in acidic canaliculi; requires ↓pH Proton Pump Inhibitor Warfarin Omeprazole GERD & PUD Hypergastrinemia (Gastric cancer?) Covalent bonds to cysteine; Take with food (Irreversible Inhibitor) Phenytoin Nocturnal Acid Breakthrough Disulfiram 24-48 hour DOA, P450 metabolism

Anti-nausea/Anti-emetic Nausea & Vomiting Constipation, Diarrhea, Headache, Oral or IV; prolonged interaction; P450 metabolism Ondansetron (5-HT3 Antagonist) (Chemotherapy induced) Lightheadedness

Hypochlorhydria, Bacterial overgrowth Benzodiazepines More stable than omeprazole; Can be given IV Proton Pump Inhibitor Warfarin Pantoprazole GERD & PUD Hypergastrinemia (Gastric cancer?) 24-48 hour DOA, P450 metabolism, requires ↓pH (Irreversible Inhibitor) Phenytoin Nocturnal Acid Breakthrough Disulfiram

Anti-emetic Vomiting Proclorperazine Choking, Drowsiness, Jaundice Depressants A depressant ( D2 Antagonist) (Chemotherapy induced) Drug Class Use Side Effects Interactions Other

Antihistamine Prevents nocturnal acid; Given orally or IV Ranitidine GERD & PUD (Reversible H2 Antagonist) Rapidly absorbed; Inhibits P450 metabolism

Aluminum Hydroxide & Sulfated Sucrose Complex Constipation Sucralfate GERD & PUD Binds & Protects gastric mucosa Decreased drug absorption Promotes prostaglandin synthesis

Fever & Malaise, Nausea & Vomiting Inhibits Arachadonic Acid Metabolism Sulfasalazine 5-aminosalicylate Mild Ulcerative Colitis Headaches, Diarrhea Scavenges reactive oxygen species Epigastric discomfort Majority of drug not absorbed

Glaucoma ( ↓ IOP) Allergic Reaction, Paraesthesia Diuretic Self-limiting (GFR feedback) Acetazolamide Epilepsy Metabolic Acidosis, Sedation, Carbonic Anhydrase Inhibitor Block Carbonic Anhydrase in proximal tubule Motion Sickness Bone Marrow Depression

Diuretics ↑ + Block epithelial Na+ channel in distal tubule Amiloride K Potassium Sparing Use with caution in diabetics Mild diuretic effect – often combined w/ 2nd diuretic

↑ Anticoagulants Ototoxic/hypotension/arrythmias ↑Lithium Diuretics Edema, CHF, Hypertension Bumetanide ↑ Uric acid, LDL & TGs & glucose ↑ Propranolol Block Na+,K+,Cl- symporter in ascending loop Loop (High Celiling) Ascites, Hypercalcemia ↑ + 2+ + - 2+ Antiarrythmals ↓ K , Ca , Na , Cl & Mg Probenecid ↓ NSAIDS ↓ Diabetes Insipidus Excess H2O retention/ Intoxication Hormone V = s. muscle contraction; V = Renal Conservation Desmopressin Acetate (Inadequate ADH Release) Intestinal cramping, vasoconstriction 1 2 Binds V & V Receptors Cutaneous Hyperstimulation 1 2 Oral or Nasal Spray Not for CAD or Renal Failure

↑ Anticoagulants Ototoxic/hypotension/arrythmias ↑Lithium Diuretics Edema, CHF, Hypertension Furosemide ↑ Uric acid, LDL & TGs & glucose ↑ Propranolol Block Na+,K+,Cl- symporter in ascending loop Loop (High Celiling) Ascites, Hypercalcemia ↑ + 2+ + - 2+ Antiarrythmals ↓ K , Ca , Na , Cl & Mg Probenecid ↓ NSAIDS ↓ ↑ Uric acid & Ca2+ / ↓ K+ & Mg2+ ↓ Anticoagulants Block Na+,Cl- symporter in distal tubule Diuretic Hypertension & Edema ↓ Uricosorics Hydrochlorthiazide ↑ (some CA inhibition) Thiazide (↓ Peripheral Vascular Resistance) LDL & TGs / ↓ Glucose tolerance ↑ Antiarrythmals Impotence & Ventricular arrythmias NSAIDS ↓ Secreted by proximal tubule cells

Diuretics Renal Failure ↓ Freely filterable, not reabsorbed Mannitol all electrolytes Osmotic Glaucoma, Cerebral Edema (K+, Ca2+, Na+, Cl- & Mg2+) Expands extracellular volume → ↑ GFR

Blocks aldosterone action at Na+,K+ATPase Diuretics Gyneomastia, Hursitism, Impotence Spironolactone Hypertension & CHF Metabolized to canrenone Potassium Sparing Decreased libido Some affinity for androgen receptors

Diuretics ↑ + Block epithelial Na+ channel in distal tubule Triamterene K Potassium Sparing Use with caution in diabetics Mild diuretic effect – often combined w/ 2nd diuretic

Doxorubicin (Adriomycin) Bleomycin ABVD Therapy Vinblastine Dacarbazine Cancer Chemotherapeutic Causes DNA Fragmentation. Complexes with FeO Minimal Myelosuppressive 2 Bleomycin Natural Products/CCS Drugs Hodgkin’s Disease Combination Therapies, Part of ABVD Regimen Pulmonary Fibrosis Antibiotic G2 Phase?

Cancer Chemotherapeutic Least myelosuppressive of Class Cisplatin Alkylating/Covalent Binding Nephrotoxic Synergize with other cancer drugs (Platinum Complex) Combination Therapy Drug Class Use Side Effects Interactions Other Cancer Chemotherapeutic Breast Carcinoma Electrophile, reacts with nucleophiles (guanine N7) Hemorrhagic Cystitis (treat w/ MESNA) Cyclophosphamide Alkylating/Covalent Binding Lymphocytic Leukemia (ALL) Hepatic Metabolism, Part of FAC Regimen Myelosuppression, Nausea, GI Ulcers (Nitrogen Mustard) Oral & IV Toxicity due to Acryline

Cancer Chemotherapeutic From Mandrake (May Apple); Synergistic w/ Platins Etoposide Natural Products/CCS Drugs Testicular Cancer Dose Limiting Myelosuppression Stimulates DNA Topoisomerase to cleave DNA Epipodophyllotoxin Blocks at S-G2

Cancer Chemotherapeutic Inhibit Pyrimidine Synthesis, Incorporated into DNA Breast Carcinoma Myelosuppression/GI Ulceration 5-Fluorouracil Antimetabolite/DNA Syn. Inhibitor Thymidilate Synthetase Inhibitor, Part of FAC Reg IV Unique Neurologic Toxicity Pyrimidine Analog Erratic Absorption;GI, Hepatic Degradation

Cancer Chemotherapeutic Only enzyme used for cancer L-Asparaginase Natural Products/CCS Drugs Hypersensitivity due to antigenicicty Depletes asparagines (inhibits protein synthesis) Enzyme Minimal BM & GI side effects

Cancer Chemotherapeutic Choriocarcinoma, Lung, Breast Reduces Folate for A,G,T synthesis (DHFR) Myelosuppression, Nausea, GI Ulcers Methotrexate Antimetabolite/DNA Syn. Inhibitor ALL, Osteosarcoma Combat toxicity with Leucovorin Cirrhosis (if chronic) Folic Acid Analog Oral Oral – Doesn’t cross BBB, Cures Choriocarcinoma Mechlorethamine Vincristine MOPP Therapy Prednisone Procarbazine Cancer Chemotherapeutic Hodgkin’s Disease, Leukemia Anti-mitotic; binds tubulin, preventing polymerization ↓ Myelosuppresion & Epithelial Vincristine Natural Products/CCS Drugs Breast Cancer Given IV (30% oral availability) Vinca Alkaloids IV ↑ NEUROTOXIC Part of MOPP

Antiplatelet Drug Acute Coronary Syndromes Abciximab Bleeding, Hypotension, Hypersensitivity Antagonize fibrinogen binding to GPIIb/IIIa GP IIb/IIIa Inhibitor Prevent restenosis after PCI

Recombinant tPA Binds fibrin – activates plasminogen Thrombolytic Acute MI (Alteplase) Given IV within 4-6 hours

Binds plasminogen, but doesn’t cleave it Streptokinase Thrombolytic Activated by deacylation of anisoyl group (Anistreplase) Inexpensive compared to tPA

Anticoagulant Inhibits fibrin bound thrombin Bivalirudin (Direct Thrombin Inhibitor) Heparin Induced Thrombocytopenia Increased Bleeding (Irreversible) Not dependent on ATIII Hirudin analog

Irreversible antagonist of platelet ADP receptor Clopidogrel Antiplatelet Drug MI Prevention & Acute Coronary Increased risk of bleeding For pts unable to tolerate aspirin (not children) (Plavix) Thienopyridines Syndromes GI Intolerance No Bone Marrow Depression

Cyanocobalamin Only organic compound with metal-carbon bond Vitamin Megaloblastic Anemia (Vitamin B12) Absorbed in ileum

Allergic-type reactions Iron Toxicity-Overload Deferoxamine Iron Chelatror Hypotension, Ear & Eye Defects Must be given slowly IV,IM or subQ Thalassemia (Histamine Involvement?)

Hypersensitivity Inhibits phosphodiesterase → ↑ cAMP Dipyridamol Antiplatelet Drug Stroke Asthma, Bronchospasm ↑ Platelet Inhibition

Bleeding, GI Intolerance Combined with aspirin; Short t1/2 Drug Class Use Side Effects Interactions Other ↑ inhibition of Xa, ↓ inhibition of Thrombin Enoxaparin Anticoagulant Clotting Easier administration (subQ), no APTT (Low Mol Wt Heparin) (Heparin) ↑ t1/2 , renal elimination, ↓ thrombocytopenia Hypertension, Seizure, Headache, Edema Stimulates erythropoiesis for HIV, renal failure, Erythropoietin Recombinant Erythropoietin Anemia Fatigue, Nausea & GI Upset Chemotherapy & frequent blood donations (Rare – more common in renal failure) Given IV or subQ, must maintain iron levels

Vitamin C ↑ Most often used, cheap Anti-Anemic GI Upset, Nausea, Heart Burn Milk ↓ Ferrous Sulfate Anemia Empty stomach = ↑ absorption, side effects (Iron) Constipation, Diarrhea Antacids ↓ Tetracycline ↓ Absorbed in duodenum & jejunum

Binds ATIII, selectively inhibits Xa Fondaparinux Anticoagulant Clotting Anemia, GI Problems Easy administration (subQ), no APTT (Pentasaccharide) (Synthetic Pentasaccharide) Prevention of DVT after knee/hip surgery Injection site reaction ↑ t1/2 (1/day dose), less preparation variability

Hypersensitivity, Hemorrhage, Enhance ATIII inhibition of IX, X & Thrombin Heparin Anticoagulant Clotting Thrombocytopenia, Osteoperosis, Short DOA, reticuloendothelial elimination (Unfractionated) (Heparin) Skin Rash Needs APTT, Binds platelets & plasma proteins

Folate Precursor Megaloblastic Anemia Leucoverin (Folic Acid) Rare Oral or IV (Converted to Tetrahydrofolate) Folate Deficiency

Binds plasminogen, but doesn’t cleave it Streptokinase Thrombolytic Activated by deacylation of anisoyl group (Anistreplase) Inexpensive compared to tPA

Urokinase Thrombolytic Acute MI Similar to Alteplase

Hemorrhage, Necrosis (loss of Protein C) Inhibits Vit. K Carboxylation Warfarin Oral Anticoagulant GI Problems, Teratogenic Many Highly protein bound, delayed onset of action Not used in liver failure Treat overdose with Vitamin K

Asthma Adrenergic Agonist Minimal (poor absorption) Overides all stimulation for bronchoconstriction Albuterol Bronchodilation/Mast Stabilization Selective  agonist Tremor ↑ HR @ high doses Prototype 2 (Early Phase)

Corticosteroid (Inhaled) Asthma Prophylaxis Oral Candidiasis (10%) Enhance lipocortin → ↓ Leukotrienes & PAF Beclomethasone (↓ COX2 & PA2) (Late Phase) Minimal systemic (poor absorption) No benefit for COPD

Antihistamine Nasal Allergies 12-24 hour DOA, Doesn’t cross BBB Cetirizine (2nd Generation) (Beginning of allergy season) Dose related drowsiness Not metabolized (Zyrtec) Antagonist of H1 Allergic Dermatoses Alter dose for liver disease

Cromolyn Sodium Unknown Antiinflammatory Asthma Prophylaxis None

Antihistamine Sedation, Dry mouth, tachycardia, Crosses BBB, suppresses cough center Diphenhydramine Nasal Allergies & Dermatoses Barbiturates (1st Generation) blurred vision, constipation, Give before histamine release, P450 Metabolism (Benadryl) Motion Sickness & Post-op Emesis Ethanol Rev, Comp Antagonist of H1 erectile dysfunction, anorexia 6 hour DOA, not for pregnant or infants

Corticosteroid (Inhaled) Asthma Prophylaxis Oral Candidiasis (10%) Fluticasone Available in different strengths (↓ COX2 & PA2) (Late Phase) Minimal systemic (poor absorption) Drug Class Use Side Effects Interactions Other Few side-effects Relieve bronchoconstriction More useful in COPD than Asthma Ipratropium Muscarinic Antagonist Minimally absorbed after inhalation COPD & Asthma Doesn’t Cross BBB Paradoxical Bronchoconstriction

Montelukast Leukotriene Receptor Antagonist Asthma Prophylaxis Unknown

Nedocromil Unknown Antiinflammatory Asthma Prophylaxis None Longer acting than Cromolyn

Adrenal Suppresion (chronic use) Corticosteroid (Oral) Prednisone Severe Asthma ↑ (↓ COX2 & PA ) Weight, ↓ glucose control, CNS effects 2 osteoporosis

Antihistamine Colds, Nausea/Vomiting Sedation & CNS effects Promethazine Barbiturates Rapid onset, 4-8 hour DOA (2nd Generation) Motion Sickness & Post-op Emesis BP Effects (Phenegran) Ethanol Sedative, anticholinergic & antiemetic effects Antagonist of H1 Parkinson’s Disease Skin Rash

Ranitidine Antihistamine Prevents nocturnal acid; Given orally or IV GERD & PUD (Zantac) (Reversible H2 Antagonist) Rapidly absorbed; Inhibits P450 metabolism

Nocturnal Asthma Prophylaxis Minimal (poor absorption) Slow onset – not for acute attacks Salmeterol Selective  agonist 2 (Early Phase) Tremor ↑ HR @ high doses Unique membrane bound drug

Asthma

Terbutaline Selective 2 agonist Bronchodilation/Mast Stabilization (Early Phase)

Methylxanthine Severe Asthma Narrow Therapeutic Index Also useful in COPD but many drug interactions Theophylline Bronchodilator Nocturnal Asthma in children Tremors, Seizures, Diuresis, Hyperglycemia, ↑ Cleared by liver/Quickly & Completely Absorbed (Limited anti-inflammatory) May increase work of diaphragm HR Oral or IV administered only – not inhaled

Thioperamide

Can inhibit P450 liver enzymes Zafirlukast Leukotriene Receptor Antagonist Asthma Prophylaxis Unknown Bioavailability decreased with food

Hyperthyroidism 131iodine (Radioactive Radiation effects (secondary cancer) Radioactive Iodine Thyroid nodule/cancer Radiation destroys parenchymal cells of thyroid Iodine) Not for young or pregnant (Oral)

Most Potent; Rapidly inactivated by liver 17b-Estradiol Natural Hormone ↑ SHBG, clotting factors, HDL, Insulin Receptors & Na+ Retention

Alpha-Glucosidase Inhibitor Acarbose Type I & II DM Abdominal Discomfort & Cramping (Inhibits  -glucosidase) Monotherapy or Combined (Precose) (Oral) Diarrhea (Blocks carb/starch absorption)

Hypoglycemia (mimics CVA) Reduce glucagons; Increase Insulin binding Acetohexamide 1st Generation Sulfonylurea Type II DM Not for renal/hepatic disease Well absorbed from GI, bound to plasma proteins (Dymelor) (Blocks ATP K+ Channels) (Oral) Not for pregnant Liver metabolism, renal excretion; Drug Class Use Side Effects Interactions Other

Cushing’s Syndrome Aminoglutethemide (Cortisol Excess)

Combined with  -2 agonists Beclomethasone Asthma (Inhaled) ↓Growth, Catacts & Bone not risks in children

Parkinson’s Disease Treatment Peritoneal Fibrosis Partial D1 agonist; ergot alkaloid Bromocryptine D2 receptor agonist Hyperprolactinemia Similar to L-DOPA Adjunct to L-DOPA (Oral) GI Upset, CNS, Insomnia Less involuntary movement than L-DOPA

Vitamin Calcitriol (↑ Ca2+/P Intestinal Absorption) Rickets/Osteomalacia (Vitamin D3) (↑ Ca2+ Bone Absorption)

Prolonged Hypoglycemia (>24 hrs) Reduce glucagons; Increase Insulin binding 1st Generation Sulfonylurea Type II DM Chlorpropamide Not for renal/hepatic disease Well absorbed from GI, bound to plasma proteins (Blocks ATP K+ Channels) (Oral) Not for pregnant Liver metabolism, renal excretion; Longest DOA

Cholecalciferol Vitamin D

Cyproterone

Syndrome of Inappropriate Demeclocycline ADH Secretion Inhibits response to ADH in collecting duct (Excess ADH Production)

Diabetes Insipidus Excess H2O retention/ Intoxication Hormone V = s. muscle contraction; V = Renal Conservation Desmopressin Acetate (Inadequate ADH Release) Intestinal cramping, vasoconstriction 1 2 Binds V & V Receptors Cutaneous Hyperstimulation 1 2 Oral or Nasal Spray Not for CAD or Renal Failure

↓ Desogestrel Synthetic Progesterone HDL:LDL, Impaired Glucose Tolerance Spotting, weight gain, acne, hirsutism

Osteoporosis, Glucose Intolerance, Cataracts, High Potency, Little effect on MR Dexamethasone Glucocorticoid Receptor Agonist Neoplasms Myopathy, Manic/Depression Better than prednisone for treating ALL ↑BP, Ulcers, Body Fat, ↓ Growth

Hypoparathyroidism (DOC) Dihydrotachysterol Vitamin D Analog Faster onset, shorter DOA than D2 or D3 Pseudohypoparathyroidism (Albrights)

Equilin Sulfate Conjugated Estrogen Hormone Replacement Therapy Enterohepatic circulation

Thrombosis, Breast & Cervical Cancer Enterohepatic circulation Ethinyl Estradiol Synthetic Estrogen Oral Contraceptives ↑ Smoking BP, ↓ Glucose Tolerance, Stroke & MI Side Effects: GI Upset, Fluid Retention, Spotting Gallbladder Disease,

Osteoporosis Etidronate Bisphosphonate Induce osteomalacia (stop mineralization) Inhibit resorption – bind hydroxyapatite Paget’s Disease Drug Class Use Side Effects Interactions Other Prostate Cancer Finasteride 4-aza testosterone analog BPH Competetively Inhibits Type II 5 Reductase Alopecia

10X higher affinity for MR than GR Hypertension Fludrocortisone Mineralocorticoid Agonist Mineralocorticoid Deficiency Monitor plasma BP & renin Hypokalemia Alternate day therapy

Non-steroidal anti-androgen Metastatic Prostate Cancer Blocks action of testosterone at receptor Flutamide (Androgen Receptor Blocker) BPH (not FDA approved) Most effective when combined with Leuprolide

Ganirelix GnRH Antagonist Hypergonadotropism

Hypoglycemia (mimics CVA) Reduce glucagons; Increase Insulin binding 2nd Generation Sulfonylurea Type II DM Glipizide Not for renal/hepatic disease Well absorbed from GI, bound to plasma proteins (Blocks ATP K+ Channels) (Oral) Not for pregnant Liver metabolism, renal excretion;

Glucagon

Hypoglycemia (mimics CVA) Reduce glucagons; Increase Insulin binding 2nd Generation Sulfonylurea Type II DM Glyburide Not for renal/hepatic disease Well absorbed from GI, bound to plasma proteins (Blocks ATP K+ Channels) (Oral) Not for pregnant Liver metabolism, renal excretion; Smaller dose

Gonadorelin Acetate GnRH Agonist

Heart Medicines Hypoglycemia & Weight Gain Better absorption than ultralente, 24 hr DOA Insulin Glargine Hormone Diabetes Ethanol Insulin Allergy; Lipo-atrophy/hypertrophy Salicylates Once daily dose at bedtime (Lantus) (Long Acting Insulin) (SubQ) Insulin Edema Pentamidine Can’t be mixed with other insulins Hormones Heart Medicines Hypoglycemia & Weight Gain Insulin Lispro Recombinant Hormone Diabetes Ethanol 2 aa’s switched in  chain; less hypoglycemia Insulin Allergy; Lipo-atrophy/hypertrophy Salicylates (Humalog) (Ultra-Short Acting Insulin) (SubQ) mimic’s normal response, dose right before meal Insulin Edema Pentamidine Hormones Osteoporosis, Glucose Intolerance, Cataracts, 1) Topical Low potency Hydrocortisone Natural Hormone Myopathy, Manic/Depression 2) Replacement Therapy Equally effective on GR & MR ↑BP, Ulcers, Body Fat, ↓ Growth Heart Medicines Hormone Hypoglycemia & Weight Gain Diabetes Ethanol Lente Insulin (Intermediate Acting Insulin with Insulin Allergy; Lipo-atrophy/hypertrophy Salicylates (SubQ) Zinc) Insulin Edema Pentamidine Hormones Androgenic

Levonorgestrel Synthetic Progesterone ↓HDL:LDL, Impaired Glucose Tolerance Most potent; Longer t1/2 Spotting, weight gain, acne, hirsutism

2+ Hypothyroidism (DOC) Avoid with Elderly & Heart Disease Ca Longer Duration Levothyroxine Sodium Fe2+ Thyroid Replacement Arrythmias & Nervousness AlOH Take on empty stomach

2+ Rapid Onset Myxedema Coma Ca Liothyronine Sodium Fe2+ Take on empty stomach (Oral & IV) AlOH Higher cost Drug Class Use Side Effects Interactions Other

2+ Liotrix Ca Fe2+ Take on empty stomach (T3 & T4 Mixture) AlOH

MedroxyProgesterone Synthetic Progesterone Longer t (Depro-Provera) 1/2

Diarrhea, Anorexia, ↓ B12 & Folate Alone or Combined; Slowly escalate dose Metformin Biguanide Type II DM Not for lactate (renal, CHF, lung, liver) No ↑ wt (may ↓); ↑HDL ↓LDL; Intestinal Absorption (Glucophage) (Inhibits Gluconeogenesis) (Oral) Don’t use with contrast dye or Creat >1.5 Doesn’t bind plasma proteins; short t1/2

Thiureylenes Methimazole Inhibits oxidation & coupling (Inhibit Thyroidperoxidase)

Selective P-450c11 Inhibitor Metyrapone Diagnostic Test of Adrenal Function Selectively inhibits cortisol production (Inhibits 11 -Hydroxylase)

Micronized Progesterone Natural Hormone IM Rapidly absorbed & metabolized to pregnanediol

Mifepristone Synthetic Progesterone Abortion Can only be used up to 7 weeks of pregnancy (RU-486) Glucocorticoid Receptor Blocker Cushing’s Disease Used in Cushing’s if etiology unknown

Alpha-Glucosidase Inhibitor Type I & II DM Monotherapy or Combined Miglitol (Inhibits  -glucosidase) (Oral) Better tolerated than Acarbose (Blocks carb/starch absorption)

Androgenic

Norethindrone Synthetic Progesterone ↓HDL:LDL, Impaired Glucose Tolerance Potent; Longer t1/2 Spotting, weight gain, acne, hirsutism

↓ Norgestimate Synthetic Progesterone HDL:LDL, Impaired Glucose Tolerance Spotting, weight gain, acne, hirsutism

Heart Medicines Hypoglycemia & Weight Gain Hormone Diabetes Ethanol NPH Insulin Insulin Allergy; Lipo-atrophy/hypertrophy Salicylates (Intermediate Acting Insulin) (SubQ) Insulin Edema Pentamidine Hormones Bind Somatostatin Receptor on Pituitary Tumor GH Excess-Acromegaly Diarrhea & Nausea Octreotide Synthetic Somatostatin Analog ↓ SubQ & IM Gallstones GH Secretion & Tumor Size Only effective on tumors with high #s of receptor

Action independent of tumor properties Pegvisomant GH Antagonist GH Excess Abnormal Liver Tests (Reversible) Inhibits receptor dimerization Monitor efficacy with IGF-1

1º = Hyperglycemia Pentamidine ??? AIDS Destroys Pancreatic -Cells 2º = Hypoglycemia (loss if insulin)

Pergolide D2 receptor agonist Hyperprolactinemia GI Upset, CNS, Insomnia Cheaper than Bromocriptine Drug Class Use Side Effects Interactions Other

Thiazolinedione (2nd gen Glitazone) Type II DM Pioglitazone (Increases # of Glut Transporters) (Oral)

Acute Eczema (oral), Ulceraritve Colitis Osteoporosis, Glucose Intolerance, Cataracts, Prednisone Glucocorticoid Receptor Agonist Graft Rejection, Neoplasms Myopathy, Manic/Depression Multiple Sclerosis, Crohn’s Disease ↑BP, Ulcers, Body Fat, ↓ Growth

Thiureylenes Agranulocytosis Inhibits oxidation, coupling & deiodination Propylthiouracil (Inhibit Thyroidperoxidase) Hyperthyroidism BM Suppression Used prior to surgical removal or radiation (Inhibits Deiodinase D1) Rash, Liver Damage

Selective Estrogen Receptor No evidence of breast/endometrial cancer Raloxifene Osteoporosis Modulator Avoids effects of 17

Heart Medicines Hypoglycemia & Weight Gain Hormone Diabetes & Ketoacidosis Ethanol Treat Ketoacidosis with low dose infusion Regular Insulin Insulin Allergy; Lipo-atrophy/hypertrophy Salicylates (Short Acting Insulin) (IV or SubQ) Treat with IV before surgery or childbirth Insulin Edema Pentamidine Hormones More potent if glc is only moderately elevated Meglitinide (Glitinide) Type II DM Hypoglycemia, Hyperinsulinemia Repaglinide Rapid onset, short DOA, taken before meals (Blocks ATP K+ Channels) (Oral) GI (uncommon) Metabolized in liver; “Dose & Eat”

URIs Once Daily Dosing; Monotherapy or combined Thiazolinedione (2nd gen Glitazone) Type II DM Rosiglitazone Headaches Requires liver testing; ↑HDL ↓LDL (Increases # of Glut Transporters) (Oral) Weight gain Delayed onset of effect; No hepatotoxicity

Less effective than Somatriptan Dwarfism Headaches, Vomiting, Intracranial HT Sermorelin Acetate Synthetic GHRH Effective in children only (SubQ) Edema, Myalgia, Arthralgia Cheaper than somatropin

Recombinant Human Headaches, Vomiting, Intracranial HT Somatropin Dwarfism/GH Deficiency Effective in children & adults Growth Hormone Edema, Myalgia, Arthralgia

Cancer Chemotherapeutic Changes in fat distribution, muscle mass Competitive Inhibitor of estrogen receptors Tamoxifen Hormone/Antihormone Mammary Carcinoma Osteoperosis Given for metastases Estrogen Deprivation Hot Flashes/Nausea

Tolbutamide

Asthma (Inhaled) Osteoporosis, Glucose Intolerance, Cataracts, Medium Potency, Little effect on MR Triamcinolone Aceonide Glucocorticoid Receptor Agonist Periarticular Inhection (Long duration) Myopathy, Manic/Depression Highly metabolized Intralesional & Joint Injections ↑BP, Ulcers, Body Fat, ↓ Growth Heart Medicines Hypoglycemia & Weight Gain Ultralente Hormone Diabetes Ethanol Insulin Isophane Insulin Allergy; Lipo-atrophy/hypertrophy Salicylates (Insulin Isophane) (Long Acting Insulin with Zinc) (SubQ) (Ultralente) Insulin Edema Pentamidine Hormones Vitamin Vitamin D (↑ Ca2+/P Intestinal Absorption) Rickets/Osteomalacia Same as Calcitriol? (↑ Ca2+ Bone Absorption)

Activated Charcoal Drug Class Use Side Effects Interactions Other DOC for Lead > 45  g/dL Calcium Disodium 1º therapy for lead poisoning (follow w/ succimer) Chelator Iron & Zinc Nephrotoxic (RT necrosis) EDTA ↓ (IV) toxicity by adequate hydration & treat < 5 days

Skin reactions Acute Iron Poisoning Deferoxamine Chelator Neuro, hepato & renal toxicity Poorly absorbed from GI (Parenteral) Histamine & Hypotensive shock

Painful Injection, Tachycardia, ↑ BP Unstable & Toxic Dimercaprol Chelator Arsenic & Acute Mercury N&V, ↑ Prothrombin time Low Therapeutic efficacy Avoid with Cadmium & Iron (renal failure)

Fomepizole Alcohol Dehydrogenase Inhibitor (4-Methylpyrazone)

Ipecac

Alcohol Methanol Metabolic acidosis & Blindness (Formate) Rx = emesis/lavage, NaBicarbonate, EtOH or Fomepizole (Industrial, Sterno, Moonshine)

N-Acetylcysteine

Copper Nephrotoxicity D-Penicillamine Chelator Well absorbed in GI (1º advantage) Adjunct for gold, lead, arsenic Autoimmune (SLE & hemolytic anemia)

More water soluble than Dimercaprol DOC for Lead GI Distress, CNS effects, skin rash Succimer Chelator High therapeutic index Also good for arsenic and mercury Liver enzyme elevation Well absorbed from GI Tract

Tissue Hypoxia (brain & Heart) Combines with hemoglobin, ↓ O2 capacity of RBC Carbon Monoxide Air Pollutant Mild CNS effects at 30-50% Hallmark is pink-cherry red skin ↓pulse & respiration at 60-70% Rx = Relieve ischemia & Pure O2 (Hyperbaric)

Air Pollutant ↑ Forms sulfurous acid on contact w/ membranes Sulfur Dioxide # mucous cells, secretion (Fossil Fuels) Bronchoconstriction Rx = Remove from exposure, provide relief

Air Pollutant Deep irritation & pulmonary edema Nitrogen Oxide Rx = Reduce irritation & edema (Fires, Silage, kerosene) Irritation to eyes, nose & throat

Shallow rapid breathing, Cough Air Pollutant Ozone Decrease in pulmonary compliance, pulmonary Rx = Reduce inflammation & edema (UV Light) edema, bronchitis

Acute = Death, corrosive to GI, bleeding Colorless and tasteless Heavy Metal Arsenic Rice water stool; Chronic = skin changes, BM Interacts with sulfhidryl groups (Environment or Industry) Depression & cancer Interferes with Pyruvate Dehydrogenase/TCA Cycle

Inhibits sulfhidryl groups ( -1-antitrypsin) Heavy Metal Inhaled = Pulmonary Edema, emphysema, Cadmium Only 5% GI absorption (Manufacturing & Fossil Fuels) nephrotoxicity; Oral = osteomalacia Rx = Chelators ineffective, Give Vitamin D

Acute = (rare) Colic & CNS changes Binds Sulfhidryl (ALA Dehydratase); Replaces Ca2+ Heavy Metal Lead Chronic = neuropathy, anorexia, anemia, Rx: >45 = chelation, <10 = prevention (Paint) tremor, GI, decreased IQ, ↓ growth Brain lags blood Drug Class Use Side Effects Interactions Other Protein precipitation, enzyme inhibition & corrosive Heavy Metal Acute: kidney & CNS, SOB, N/V & chest Mercury Binds functional groups; Methyl is worst (Fish, Fungicides & Air Pollution) pain; Chronic: CNS & GI Rx = penicillamine & DMSA

Acute: N/V, bleeding, lethargy, pneumonitis & Heavy Metal GI corrosion/ulceration, necrosis Iron seizures, tachycardia, hepatic failre, ↑ SGOT & (Vitamins) ↓ SGPT cardiac fxn, hepatic damage

Acidosis: MeOH>Et Glycol>EtOH>IPA Ethanol Alcohol Ketoacidosis ↑ Anion gap Rx = avoid stimulants, correct electrolytes/sugar

Alcohol Methanol Metabolic acidosis & Blindness (Formate) Rx = emesis/lavage, NaBicarbonate, EtOH or Fomepizole (Industrial, Sterno, Moonshine)

Calcium Oxalate damge to kidneys Metabolites more toxic than parent Alcohol Ethylene Glycol Pulmonary edema, CHF, Tachycardia Inhibits oxidative phosphorylation (Antifreeze) Renal Failure, N/V Rx = NaBicarb, ethanol or fomepizole

Halogenated Hydrocarbons sensitize heart to Pulmonary(worst): Pneumonitis, Hemorrhagic Hydrocarbons Hydrocarbons catecholamines & arrythmias bronchopneumonia, CNS, GI, Hepatic & Heart Rx: prevent aspiration, emesis, support

Acetylcholine Muscarinic/Cholinergic Agonist None - naturally occuring Hypotension, Multiple PNS Effects Not effective orally - short duration (ChE)

Mad, Hot, Blind, Dry, Red Muscarinic Antagonist AChE Inhibitor Antidote PNS & CNS Atropine Treat OD with physostigmine (Jimson weed) Inhibits M receptors in PNS/CNS Can cause glaucoma crisis (↑ IOP) Crosses BBB

Low Dose: Stimulate ganglia CNS (stimulate or depress), PNS, NMJ Metabolized by liver, Excretion pH dependent Nicotine Ganglionic (Nicotinic) Agonist High Dose: Block ganglia Stimulates Carotid Body Receptors Crosses BBB

Low Dose: Vasodilation (  ) Anaphylaxis 2 Not given orally – metabolized Epinephrine Adrenergic Agonist High Dose: Vasoconstriction ( ) Shock & Bronchodilation DOC for anaphylaxis Can cause hypertension

Adrenergic Agonist Limited clinical use Norepinephrine Can cause hypertension Not given orally - metabolized (Low affinity for 2) (Neurotransmitter)

CHF & Shock Adrenergic Agonist Not given orally - metabolized Dopamine Renal vasodilation ( DA1) Arrythmias & ↑ TPR (OD) DA >  >  >  Short t 1 1 1 2 ↑ Myocardial contraction (not rate) ½

↑ inhibition of Xa, ↓ inhibition of Thrombin Anticoagulant LMW Heparin Clotting Easier administration (subQ), no APTT (Heparin) ↑ t1/2 , renal elimination, ↓ thrombocytopenia Excess H2O retention/ Intoxication Natural Hormone Diabetes Insipidus Vasopressin Intestinal cramping, vasoconstriction V = s. muscle contraction; V = Renal Conservation Binds V & V Receptors (Inadequate ADH Release) 1 2 1 2 Not for CAD or Renal Failure Drug Class Use Side Effects Interactions Other Vitamin C ↑ More expensive, Complex preparations Anti-Anemic Milk ↓ Ferrous gluconate Anemia Fewer than ferrous sulfate Empty stomach = ↑ absorption, side effects (Iron – Organic Salt) Antacids ↓ Tetracycline ↓ Absorbed in duodenum & jejunum

Hydroxycibalamin Only organic compound with metal-carbon bond Vitamin Megaloblastic Anemia (Vitamin B12) Absorbed in ileum

Contraceptives ↓ Antifolates ↓ Folic Acid Vitamin Megaloblastic Anemia Anticonvulsants ↓ Absorbed in jejunum Antiepileptics ↓

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