Drug Receptor Types

Functions of Peripheral Adrenergic Receptor Subtypes
Receptor Subtype Alpha1 Location Eye Arterioles (skin, viscera, mucous membranes) Veins Sex organs, male Bladder neck and prostatic capsule Presynaptic nerve terminals Heart Kidney Arterioles (heart, lung, and skeletal mucle) Bronchi Uterus Liver Skeletal muscle Kidney Response to Receptor Activation Mydriasis—wide eyed with fear Constriction Constriction Ejaculation Contraction Inhibition of transmitter release—decreases sympathetic nervous system (SNS) outflow to the blood vessels and heart Increased rate, force of contraction, and AV conduction velocity Renin release—RAS Dilation Dilation Relaxation Glycogenolysis Enhanced contraction, glycogenolysis Dilation of kidney vasculature

Functions of Peripheral Cholinergic Receptor Subtypes
Receptor Subtype Nicotinicn Location All autonomic nervous system ganglia and the adrenal medulla Response to Receptor Activation Stimulation of parasympathetic and sympathetic postganglionic nerves and release of epinephrine from the adrenal medulla Contraction of skeletal muscle Miosis Decreased rate Constriction of bronchi Promotion of secretions Voiding Salivation Increases gastric secretions, intestinal tone, and motility Defecation Generalized sweating Erection Vasodilation

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Alpha2 Beta1 Beta2

Nicotinicm Neuromuscular junction Muscarinic All parasympathetic target organs: Eye Heart Lung Bladder GI tract

Dopamine

Sweat glands Sex organs Blood vessels

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Drug Endings
Drug Endings -zosin -olol, -lol -zepam, -zolam -pril -artan -dipine -statin -ase, -plase -parin -sone -dronate Drug Classification Alpha-adrenergic blocker Beta-adrenergic blocker Benzodiazepine (BZD) Angiotensin-converting enzyme (ACE) inhibitor Angiotensin-receptor blocker (ARB) Calcium channel blocker Lipid-lowering drug Thrombolytic Anticoagulant Corticosteroid Bisphosphonate for osteoporosis Drug Example prazosin metoprolol diazepam, alprazolam lisinopril candesartan amlodipine atorvastatin alteplase enoxaparin prednisone alendronate Continued Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

Drug Endings—cont’d
Drug Endings -terol -tidine -prazole -cillin -cef, -ceph -cycline -floxacin -thromycin -micin, -mycin -azole Drug Classification Bronchodilator Histamine2 blocker–acid reducer Protein pump inhibitor–acid reducer Penicillin antibiotic Cephalosporin antibiotic Tetracycline antibiotic Fluoroquinolone antibiotic Macrolide antibiotic Aminoglycoside antibiotic Antifungal Drug Example albuterol cimetidine omeprazole amoxicillin cefazolin tetracycline levofloxacin azithromycin gentamycin itraconazole

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BETHANECHOL (URECHOLINE) Muscarinic Agonist

BETHANECHOL (URECHOLINE) Muscarinic Agonist
Activates muscarinic receptors Causes contraction of the detrusor muscle of the bladder

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Uses Postoperative urinary retention Adverse Effects Hypotension Bradycardia, dysrhythmias Bronchoconstriction GI effects

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ATROPINE Muscarinic Antagonist (Anticholinergic)

ATROPINE Muscarinic Antagonist (Anticholinergic)
Blocks muscarinic receptors Increases heart rate Decreases salivary, bronchial, sweat, and acid-secreting cell secretions Relaxes bronchial smooth muscles Decreases bladder tone and GI motility Dilates pupils (mydriasis)

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Uses Preanesthesia to prevent bradycardia, treatment of bradycardia Dilation of pupil for ocular examination or surgery Intestinal hypertonicity and hypermotility Antidote for muscarinic-agonist poisoning Adverse Effects
Blurry vision, urinary retention, dry mouth, constipation, tachycardia Increases intraocular pressure

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NEOSTIGMINE (PROSTIGMINE) Reversible Cholinesterase Inhibitor

NEOSTIGMINE (PROSTIGMINE) Reversible Cholinesterase Inhibitor
Prevents the degradation of acetylcholine (ACh) Enhances the effect of ACh to stimulate skeletal muscle

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Uses Myasthenia gravis Reversal of neuromuscular blockade in postoperative patients Adverse Effects Excessive glandular secretions, increased GI motility Urinary urgency, bradycardia, sweating, and miosis Cholinergic crisis—treat with atropine

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SUCCINYLCHOLINE Depolarizing Neuromuscular Blocker

SUCCINYLCHOLINE Depolarizing Neuromuscular Blocker
Causes paralysis of muscle by preventing repolarization

Uses

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Muscle relaxation during endotracheal intubation Used for short operative procedures

Adverse Effects
Prolonged paralysis in genetically determined individuals Malignant hyperthermia—treat with dantrolene Muscle pain, hyperkalemia

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PHENYLEPHRINE Adrenergic Agonist

PHENYLEPHRINE Adrenergic Agonist
Activates alpha1 receptors Constricts blood vessels of the skin, viscera, and mucous membranes

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Uses Treatment of nasal congestion Delay of anesthetic absorption Dilation of the pupil for ocular exam Adverse Effects Hypertension Necrosis

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EPINEPHRINE Adrenergic Agonist (Catecholamine)

EPINEPHRINE Adrenergic Agonist (Catecholamine)
Activates all four adrenergic receptors—alpha1, alpha2, beta1, and beta2 Pupil dilation, arterial and venous vasoconstriction Increases heart rate and force of contraction Bronchial dilation, glycogenolysis, enhanced muscle contraction

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Uses
Cardiac arrest, heart failure, and anaphylactic shock AV heart block and asthma Delays absorption of local anesthetic and controls superficial bleeding Reduces nasal congestion Dilates pupil for eye procedures

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Adverse Effects Hypertension, tachycardia, and dysrhythmias Angina, necrosis following extravasation Hyperglycemia in diabetic patients

PROPRANOLOL (INDERAL) Adrenergic Antagonist Noncardioselective Beta Blocker
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PROPRANOLOL (INDERAL) Adrenergic Antagonist Noncardioselective Beta Blocker
Blocks beta1 and beta2 receptors Reduces heart rate, decreases force of ventricular contraction Decreases conduction through AV node, decreases cardiac output Suppresses renin, bronchoconstriction

Uses
Angina, hypertension, cardiac dysrhythmias Myocardial infarction, heart failure, hyperthyroidism, glaucoma

Adverse Effects
Bradycardia, reduced cardiac output, AV heart block Rebound cardiac excitation, bronchoconstriction Inhibition of glycogenolysis, CNS effects Not used in patients with asthma or diabetes

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METOPROLOL (LOPRESSOR, TOPROL XL) Adrenergic Antagonist Cardioselective Beta Blocker
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METOPROLOL (LOPRESSOR, TOPROL XL) Adrenergic Antagonist Cardioselective Beta Blocker
Blocks cardiac beta1 receptors Reduces heart rate, decreases force of ventricular contraction Decreases conduction through AV node, decreases cardiac output Suppresses renin Does not block beta2 receptors (no bronchoconstriction) Not likely to inhibit glycogenolysis Preferred for patients with asthma or diabetes

Uses
Hypertension, angina pectoris, heart failure

Adverse Effects
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Bradycardia, reduction of cardiac output, AV heart block Rebound cardiac excitation following abrupt withdrawal

PRAZOSIN (MINIPRESS) Adrenergic Antagonist Alpha Blocker
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PRAZOSIN (MINIPRESS) Adrenergic Antagonist Alpha blocker
Blocks alpha1 receptors Dilates arteries and veins Relaxes smooth muscle in the bladder neck and prostatic capsule

Uses Hypertension Benign prostatic hypertrophy Adverse Effects Orthostatic hypotension, reflex tachycardia Inhibition of ejaculation Nasal congestion Use with sildenafil (Viagra), other drugs for erectile dysfunction, can lead to hypotension

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CLONIDINE (CATAPRES) Centrally Acting Alpha2 Agonist Antihypertensive Drug
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CLONIDINE (CATAPRES) Centrally Acting Alpha2 Agonist Antihypertensive Drug
Activates alpha2 receptors in the CNS Reduces sympathetic flow to the heart and blood vessels Reduces stimulation of adrenergic receptors in the periphery Net effect of cardiac suppression and vasodilation is decreased blood pressure

Uses
Hypertension

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Adverse Effects Hypotension Bradycardia, decrease in cardiac output Drowsiness, dry mouth Rebound hypertension in response to abrupt withdrawal Fetal harm

LEVODOPA/CARBIDOPA (SINEMET) Dopaminergic Agent

LEVODOPA/CARBIDOPA (SINEMET) Dopaminergic Agent
Levodopa increases synthesis of dopamine in the striatum Carbidopa enhances the effect of levodopa

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Uses Reduces symptoms of Parkinson’s disease Adverse Effects Effects take several months to develop Loss of effect occurs over time Nausea, vomiting, dyskinesias Postural hypotension, psychosis Dark sweat and urine, may activate melanoma

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DONEPEZIL (ARICEPT) Cholinesterase Inhibitor

DONEPEZIL (ARICEPT) Cholinesterase Inhibitor
Prevents the breakdown of ACh Increases ACh at cholinergic synapses May slow progression of Alzheimer’s disease (AD) Some improvement of cognitive function

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Uses Alzheimer’s disease (AD) Adverse Effects Cholinergic effects Nausea, vomiting, dyspepsia, diarrhea Bradycardia, bronchoconstriction

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PHENYTOIN (DILANTIN) Antiepileptic Drug (AED)

PHENYTOIN (DILANTIN) Antiepileptic Drug (AED)
Inhibits entry of sodium into neurons Suppresses action potential of neurons

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Uses Epilepsy Adverse Effects Nystagmus, sedation, ataxia, diplopia Cognitive impairment, gingival hyperplasia, hirsutism Rash, fetal harm, bleeding tendencies in newborns Narrow therapeutic range (10 to 20 mcg/mL) Can decrease the effect of other drugs such as: Oral contraceptives, warfarin, and glucocorticoids Inject slowly, use normal saline flush Withdraw over a period of 6 to 8 weeks to avoid seizures

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VALPROIC ACID (DEPAKOTE) Antiepileptic Drug (AED)

VALPROIC ACID (DEPAKOTE) Antiepileptic Drug (AED)
Blocks sodium channels to suppress neurons Suppresses calcium influx Increases inhibitory influence of gamma-aminobutyric acid (GABA)

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Uses Epilepsy, bipolar disorder, migraine headaches Adverse Effects
Nausea, vomiting, indigestion Hepatotoxicity, pancreatitis, fetal harm Weight gain, rash, hair loss, tremor Blood dyscrasias

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MORPHINE Opioid Analgesic

MORPHINE Opioid Analgesic
Activates mu receptors Produces analgesia, euphoria, sedation

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Uses Relief of pain Adverse Effects Respiratory depression, constipation Orthostatic hypotension, urinary retention, miosis Biliary colic, euphoria, sedation, cough suppression Tolerance and physical dependence Reversed with naloxone (Narcan)

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NALOXONE (NARCAN) Opioid Antagonist

NALOXONE (NARCAN) Opioid Antagonist
Reverses the effects of opioids

Uses

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Opioid overdose Reversal of excessive respiratory depression

Adverse Effects Minimal

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SUMATRIPTAN (IMITREX) Serotonin1B/1D-Receptor Agonist (Triptan)

SUMATRIPTAN (IMITREX) Serotonin1B/1D-Receptor Agonist (Triptan)
Binds to 5-HT1B/1D receptors to cause vasoconstriction Reduces release of inflammatory peptides Diminishes perivascular inflammation

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Uses
Migraine headache

Adverse Effects Chest pressure, coronary vasospasm Fetal harm

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CONVENTIONAL ANTIPSYCHOTICS (NEUROLEPTICS)
Chlorpromazine (Thorazine) Thioridazine (Mellaril) Haloperidol (Haldol)

CONVENTIONAL ANTIPSYCHOTICS (NEUROLEPTICS)
Relieve positive symptoms of schizophrenia Block receptors for dopamine, acetylcholine (ACh), histamine, and norepinephrine (NE)

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Uses Schizophrenia, bipolar disorder, Tourette’s syndrome, and dementia Adverse Effects Extrapyramidal symptoms (EPS) (acute dystonia, parkinsonism, akathisia, tardive dyskinesia) Neuroleptic malignant syndrome Anticholinergic effects, orthostatic hypotension Sedation, neuroendocrine effects, seizures Sexual dysfunction, increased risk of sunburn Agranulocytosis, dysrhythmias

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ATYPICAL ANTIPSYCHOTICS
Clozapine (Clozaril) Risperidone (Risperdal) Olanzapine (Zyprexa) Quetiapine (Seroquel) Ziprasidone (Geodon) Aripiprazole (Abilify)

ATYPICAL ANTIPSYCHOTICS
Relieve positive and negative signs and symptoms of schizophrenia Block receptors for serotonin, dopamine, ACh, histamine, and NE Clinically superior to conventional antipsychotics

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Uses Schizophrenia Adverse Effects
Sedation, orthostatic hypotension, weight gain, dry mouth Blurry vision, urinary retention, constipation, tachycardia Galactorrhea, gynecomastia, amenorrhea, diabetes Agranulocytosis, seizures Low risk of extrapyramidal effects

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SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs)
Fluoxetine (Prozac) Paroxetine (Paxil) Sertraline (Zoloft) Citalopram (Celexa) Escitalopram (Lexapro)

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs) Antidepressants
Inhibit serotonin reuptake (more serotonin is available at the synapse)

Antidepressants

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Uses Major depression, OCD Panic disorder, PTSD, PMDD Adverse Effects Sexual dysfunction, nausea, headache, insomnia Weight gain, serotonin syndrome Withdrawal syndrome

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TRICYCLIC ANTIDEPRESSANTS (TCAs)
Amitriptyline (Elavil) Clomipramine (Anafranil) Desipramine (Norpramin) Doxepin (Sinequan)

TRICYCLIC ANTIDEPRESSANTS (TCAs) Antidepressants
Inhibit reuptake of NE and serotonin (more serotonin and NE available at the synapse)

Antidepressants

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Uses Depression, bipolar disorder, insomnia, and neuropathic pain Adverse Effects Orthostatic hypotension, sedation Anticholinergic effects Cardiotoxicity, seizures, hypomania Many drug interactions SSRIs preferred for treatment of depression

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MONOAMINE OXIDASE INHIBITORS (MAOIs) Antidepressants

MONOAMINE OXIDASE INHIBITORS (MAOIs) Antidepressants
Increase NE and serotonin by blocking enzyme that inactivates them

Uses

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Depression

Adverse Effects CNS stimulation, orthostatic hypotension Hypertensive crisis from buildup of dietary tyramine Many drug interactions SSRIs preferred for treatment of depression

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LITHIUM Mood-Stabilizing Drug

LITHIUM Mood-Stabilizing Drug
Mechanism unclear, may alter ions and neurotransmitters

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Uses Stabilizes mood in patients with bipolar disorder Reduces euphoria, hyperactivity, and other symptoms Preferred for patients with classic (euphoric) mania Adverse Effects
Accumulates to toxic levels in the presence of a low sodium level Lithium levels must be kept below 1.5 mEq/L Blood levels drawn 12 hours after evening dose Signs of toxicity include fine hand tremor, GI upset, thirst, polyuria, and muscle weakness Chronic use can lead to renal toxicity and hypothyroidism Pregnancy Risk Category D Drug interactions occur with diuretics, NSAIDs, and anticholinergics

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VALPROIC ACID (DEPAKOTE) Mood-Stabilizing Anticonvulsant

VALPROIC ACID (DEPAKOTE) Mood-Stabilizing Anticonvulsant
Suppresses mania and stabilizes mood

Uses

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Mood stabilizer for patients with bipolar disorder

Adverse Effects GI disturbances, weight gain Rare thrombocytopenia, pancreatitis, liver failure Target trough level is 50 to 125 mg/mL

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LAMOTRIGINE (LAMICTAL) Newer Mood-Stabilizing Anticonvulsant

LAMOTRIGINE (LAMICTAL) Newer Mood-Stabilizing Anticonvulsant
Shows some efficacy in treating bipolar disorder

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Uses Bipolar disorder Adverse Effects
Headache, dizziness, double vision Life-threatening rashes include Stevens-Johnson syndrome and epidermal necrolysis

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BENZODIAZEPINES (BZDs)
Alprazolam (Xanax) Diazepam (Valium) Flurazepam (Dalmane) Lorazepam (Ativan) Midazolam (Versed) Temazepam (Restoril)

BENZODIAZEPINES (BZDs) Sedative Hypnotic Drugs
Depress central nervous system function Reduce anxiety, promote sleep Potentiate the actions of GABA (an inhibitory neurotransmitter)

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Sedative-Hypnotic Drugs

Uses Anxiety, insomnia, seizure disorder, induction of anesthesia Muscle spasm, panic disorder, and withdrawal from alcohol Adverse Effects CNS depression, anterograde amnesia, paradoxic effects Weak respiratory depression if given orally IV administration can cause severe respiratory depression Abuse and addiction, teratogenic Do not mix with other CNS depressants or alcohol Reversal agent is flumazenil (Romazicon)

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ZOLPIDEM (AMBIEN) ZALEPLON (SONATA) Sedative-Hypnotics BZD-like Drugs
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ZOLPIDEM (AMBIEN) Sedative-Hypnotics BZD-like Drugs
Potentiate the actions of GABA (an inhibitory neurotransmitter)

Uses
Short-term management of insomnia

Adverse Effects
Daytime drowsiness, dizziness Do not use with alcohol or other CNS depressants

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BARBITURATES
Thiopental (Pentothal) Secobarbital (Seconal) Phenobarbital

BARBITURATES CNS Depressants
Potentiate the actions of GABA (an inhibitory neurotransmitter)

Uses

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CNS Depressants

Insomnia Suppression of seizures, induction of general anesthesia

Adverse Effects
Respiratory depression, decreased blood pressure and heart rate Induction of hepatic drug-metabolizing enzymes (increases the metabolism of other drugs) May lead to tolerance and dependence Frequently used as vehicles for suicide Teratogenic

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METHYLPHENIDATE (RITALIN, METADATE, CONCERTA) CNS Stimulant for ADHD
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METHYLPHENIDATE (RITALIN, METADATE, CONCERTA) CNS Stimulant for ADHD
Promotes norepinephrine (NE) and dopamine (DA) release Inhibits NE and DA reuptake

Uses Attention deficit/hyperactivity disorder (ADHD) Narcolepsy Adverse Effects Insomnia, reduced appetite, palpitations, hypertension, angina, dysrhythmias, psychosis Abrupt discontinuation can lead to withdrawal reactions Potential for abuse (Schedule II) Sudden death

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ATOMOXETINE (STRATTERA) Nonstimulant Drug for ADHD

ATOMOXETINE (STRATTERA) Nonstimulant Drug for ADHD
Selective inhibitor of NE reuptake Causes NE to accumulate at synapses

Uses

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ADHD in children and adults

Adverse Effects
GI reactions, reduced appetite, dizziness, and somnolence Urinary retention, mood swings, insomnia, sexual dysfunction

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ADDERALL CNS Stimulant Used for ADHD Combination Amphetamine
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ADDERALL CNS Stimulant Used for ADHD Combination Amphetamine
Uses
ADHD

Adverse Effects Insomnia, growth suppression Headache, abdominal pain, lethargy Abuse potential (Schedule II) Sudden death Drug holidays recommended

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DISULFIRAM (ANTABUSE) Aversion Therapy for Alcoholism

DISULFIRAM (ANTABUSE) Aversion Therapy for Alcoholism
Disrupts alcohol metabolism by blocking enzyme Aldehyde accumulates and produces unpleasant effects

Uses

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Alcohol abuse

Adverse Effects
Nausea, vomiting, flushing, palpitations, headache Sweating, blurry vision, hypotension, chest pain, shock will occur with 7 mL of alcohol ingestion

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FUROSEMIDE (LASIX) Loop Diuretic

FUROSEMIDE (LASIX) Loop Diuretic
Blocks reabsorption of sodium and chloride in the descending limb of the loop of Henle to promote urination Produces profound diuresis

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Uses
Rapid mobilization of fluid Pulmonary edema resulting from heart failure or renal or liver disease Especially useful in patients with renal insufficiency

Adverse Effects
Hypokalemia, hyponatremia, hypochloremia, dehydration, hypotension, and ototoxicity May cause dysrhythmias when used with digoxin (decreases potassium)
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HYDROCHLOROTHIAZIDE (HCTZ) Thiazide Diuretic

HYDROCHLOROTHIAZIDE (HCTZ) Thiazide Diuretic
Blocks reabsorption of sodium and chloride in the early segment of the distal convoluting tubule to promote urination

Uses

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Treatment of hypertension Mobilization of edema with mild heart failure, hepatic or renal disease

Adverse Effects
Hyponatremia, hypochloremia, dehydration Hypokalemia and hypotension

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SPIRONOLACTONE (ALDACTONE) Potassium-Sparing Diuretic

SPIRONOLACTONE (ALDACTONE) Potassium-Sparing Diuretic
Blocks the actions of aldosterone in the distal nephron Causes the retention of potassium and increased excretion of sodium

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Uses Hypertension and edema Heart failure Primary hyperaldosteronism Adverse Effects
Endocrine effects such as: Gynecomastia, menstrual irregularities, impotence, and hirsutism Hyperkalemia

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ENALAPRIL (VASOTEC)
Benazepril (Lotensin) Fosinopril (Monopril) Lisinopril (Prinivil and Zestril) Moexipril (Univasc) Perindopril (Aceon) Quinapril (Accupril) Ramipril (Altace) Trandolapril (Mavik)

ENALAPRIL (VASOTEC) Angiotensin-Converting Enzyme (ACE) Inhibitor
Inhibits ACE, reducing levels of angiotensin II Dilates arterioles and veins to reduce BP Reduces blood volume

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Uses Hypertension, heart failure, MI, diabetic nephropathy Prevention of MI, stroke, and death Adverse Effects Hypotension, cough, hyperkalemia Renal failure in patients with renal artery stenosis Fetal injury Angioedema

Angiotensin-Converting Enzyme (ACE) Inhibitors

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LOSARTAN (COZAAR)
Candesartan (Atacand) Eprosartan (Teveten) Olmesartan (Benicar) Telmisartan (Micardis) Valsartan (Diovan)

LOSARTAN (COZAAR) Angiotensin II-Receptor Blocker (ARB)
Blocks the actions of angiotensin II Dilates arterioles and veins to reduce BP Reduces blood volume

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Uses
Hypertension, heart failure, MI, and diabetic nephropathy Prevention of MI, stroke, and death

Angiotensin II-Receptor Blockers (ARBs)

Adverse Effects
Renal failure in patients with renal artery stenosis Hypotension Angioedema Fetal injury Does not cause cough or hyperkalemia

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VERAPAMIL (CALAN) DILTIAZEM (CARDIZEM) Calcium Channel Blockers (CCBs) Nondihydropyridines
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VERAPAMIL (CALAN) DILTIAZEM (CARDIZEM) Calcium Channel Blockers (CCBs) Nondihydropyridines
Block calcium channels in the heart and blood vessels Reduce BP by blocking calcium channels in the arterioles Increase coronary perfusion Block SA and AV nodes to reduce heart rate and contractility Decrease force of contraction

Uses Angina, hypertension, cardiac dysrhythmias Adverse Effects
Constipation, dizziness, facial flushing, edema, hypotension Bradycardia, AV block, decreased cardiac contractility

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AMLODIPINE (NORVASC) Calcium Channel Blocker Dihydropyridine
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AMLODIPINE (NORVASC) Calcium Channel Blocker Dihydropyridine
Blocks calcium channels in the blood vessels Vasodilation in peripheral arterioles lowers blood pressure

Uses Hypertension Angina Adverse Effects Peripheral edema, flushing, dizziness, headache Does not slow heart rate like nondihydropyridines

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DIGOXIN (LANOXIN) Cardiac Glycoside Positive Inotropic Agent Drug for Heart Failure
Increases the force of ventricular contraction Inhibits Na , K -ATPase to increase Ca inside myocytes Competes with K for binding to Na , K -ATPase ↓K → ↑ Na , K -ATPase inhibition → digoxin toxicity Changes electrical activity of the heart and slows heart rate

DIGOXIN (LANOXIN) Cardiac Glycoside Positive Inotropic Agent Drug for Heart Failure
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Uses
Heart failure and dysrhythmias

Adverse Effects
Anorexia, nausea and vomiting, fatigue Visual disturbances (blurry vision, yellow tinge, halos) Dysrhythmias Digoxin toxicity (therapeutic level 0.5 to 0.8 ng/mL) Hold if HR 60 BPM or K is low Inject slowly over 5 minutes Give Digibind for digoxin overdose

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AMIODARONE (CORDARONE) Antidysrhythmic Class III Potassium Channel Blocker
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AMIODARONE (CORDARONE) Antidysrhythmic Class III Potassium Channel Blocker
Delays repolarization Reduces automaticity in the SA node, reduces contractility Decreases conduction velocity in the AV node, ventricles, and His-Purkinje system

Uses
Recurrent ventricular fibrillation Unstable ventricular tachycardia

Adverse Effects
Widening of the QRS complex Prolongation of the PR and QT intervals Pulmonary toxicities, sinus bradycardia, AV block, hypotension Corneal microdeposits, optic neuropathy Hepatitis, thyroid dysfunction Toxicities in pregnancy Grapefruit juice increases levels to toxicity

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VERAPAMIL (CALAN) DILTIAZEM (CARDIZEM) Antidysrhythmics Class IV Calcium Channel Blockers
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VERAPAMIL (CALAN) DILTIAZEM (CARDIZEM) Antidysrhythmics Class IV Calcium Channel Blockers
Block calcium channels in the heart Slow SA node automaticity, delay AV nodal conduction Reduce myocardial contractility

Uses
Atrial fibrillation or atrial flutter Supraventricular tachycardia

Adverse Effects
Bradycardia, AV block, and heart failure Hypotension, peripheral edema, and constipation Can elevate digoxin levels Grapefruit juice increases levels to toxicity

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PROCAINAMIDE (PRONESTYL) Antidysrhythmic Class IA Sodium Channel Blocker
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PROCAINAMIDE (PRONESTYL) Antidysrhythmic Class IA Sodium Channel Blocker
Blocks cardiac sodium channels Slows conduction in the atria, ventricles, and His-Purkinje system Delays depolarization

Uses Atrial and ventricular dysrhythmias Adverse Effects Systemic lupus erythematous–like syndrome Blood dyscrasias QRS widening and prolongation

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LIDOCAINE (XYLOCAINE) Antidysrhythmic Class IB Sodium Channel Blocker
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LIDOCAINE (XYLOCAINE) Antidysrhythmic Class IB Sodium Channel Blocker
Blocks cardiac sodium channels Slows conduction in the atria, ventricles, and His-Purkinje system Reduces automaticity in the ventricles and His-Purkinje system Accelerates repolarization

Uses Short-term therapy for ventricular dysrhythmias Adverse Effects
No significant impact on the ECG Drowsiness, confusion, and paresthesias Toxic doses may produce convulsions and respiratory arrest

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PROPRANOLOL (INDERAL) Antidysrhythmic Class II Beta Blocker
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PROPRANOLOL (INDERAL) Antidysrhythmic Class II Beta Blocker
Beta-adrenergic antagonist Blocks both beta1 and beta2 receptors Decreases automaticity of the SA node Decreases velocity of conduction through the AV node Decreases myocardial contractility

Uses Sinus tachycardia, severe recurrent ventricular tachycardia Paroxysmal atrial tachycardia, hypertension Adverse Effects Prolongs PR interval on the ECG Bradycardia, heart failure, AV block, and sinus arrest Bronchospasm in patients with asthma

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ATORVASTATIN (LIPITOR) FLUVASTATIN (LESCOL) LOVASTATIN (MEVACOR) PRAVASTATIN (PRAVACHOL) SIMVASTATIN (ZOCOR) ROSUVASTATIN (CRESTOR)
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ATORVASTATIN (LIPITOR) Lipid-Lowering Drug HMG-CoA Reductase Inhibitor (Statin)
Inhibits the enzyme that synthesizes cholesterol Increases the number of LDL receptors to remove LDL Slows progression of CHD, stabilizes plaque

Lipid-Lowering Drugs HMG-CoA Reductase Inhibitors (Statins)

Uses
Hypercholesterolemia Primary prevention of CHD

Adverse Effects
Hepatotoxicity, increases ALT and AST Myopathy, increases CK levels, rhabdomyolysis, dark urine, renal failure Pregnancy Risk Category X Headache, rash, GI complaints Cyclosporine, macrolide antibiotics, azole antifungals, and HIV protease inhibitors raise some statins to toxic levels

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NICOTINIC ACID (NIACIN) Lipid-Lowering Agent

NICOTINIC ACID (NIACIN) Lipid-Lowering Agent
Reduces LDL and triglycerides Increases HDL

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Uses Dyslipidemia Adverse Effects Hepatotoxicity Flushing, itching Gastric upset, nausea, vomiting, diarrhea May raise blood sugar in patients with diabetes May increase incidence of gout

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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CHOLESTYRAMINE (QUESTRAN) COLESEVELAM (WELCHOL) Bile-Acid Sequestrants
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CHOLESTYRAMINE (QUESTRAN) Bile-Acid Sequestrant
Forms insoluble complex with bile acids Increases LDL receptors Safest of all lipid-lowering drugs

Uses Hypercholesterolemia Often used in combination with statin Adverse Effects Constipation, bloating, indigestion Reduces uptake of fat-soluble vitamins Interferes with absorption of other drugs

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

GEMFIBROZIL (LOPID) FENOFIBRATE (TRICOR) Fibric Acid Derivatives (Fibrates)
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GEMFIBROZIL (LOPID) Fibric Acid Derivative (Fibrate)
Decreases triglycerides by lowering VLDL Raises HDL levels

Uses Hypertriglyceridemia Adverse Effects Myopathy, liver injury Rash, nausea, abdominal pain, diarrhea Gallstone formation Increases warfarin levels, leading to hemorrhage

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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EZETIMIBE (ZETIA) Cholesterol-Lowering Drug

EZETIMIBE (ZETIA) Cholesterol-Lowering Drug
Blocks cholesterol absorption in the small intestine

Uses

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Hypercholesterolemia Used in combination with statins

Adverse Effects
May increase risk of liver damage when used with statin May increase risk of gallstone formation

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

NITROGLYCERINE Organic Nitrate

NITROGLYCERINE Organic Nitrate
Dilates veins, decreases venous return to the heart Decreases preload Decreases cardiac oxygen demand

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Uses
Angina, myocardial infarction

Adverse Effects Headache, orthostatic hypotension Reflex tachycardia Use with sildenafil (Viagra), other drugs for erectile dysfunction may lead to severe hypotension

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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CLOPIDOGREL (PLAVIX) Adenosine Diphosphate–Receptor Antagonist ADP Receptor Blocker Antiplatelet Drug
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CLOPIDOGREL (PLAVIX) Adenosine Diphosphate–Receptor Antagonist ADP Receptor Blocker Antiplatelet Drug
Blocks enzyme so that platelets are unable to aggregate

Uses Prevention of stroke and MI Adverse Effects Hemorrhage

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

EPTIFIBATIDE (INTEGRILIN) Glycoprotein llb/llla–Receptor Antagonists Antiplatelet Drug—”Super Aspirin”
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EPTIFIBATIDE (INTEGRILIN) Glycoprotein llb/llla–Receptor Antagonists Antiplatelet Drug—”Super Aspirin”
Interferes with the final step in platelet aggregation

Uses
Acute coronary syndrome Used during angioplasty

Adverse Effects
Intercranial hemorrhage, gastrointestinal bleeding Hematuria, gingival bleeding Thrombocytopenia Anaphylaxis

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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ALTEPLASE (tPA) Thrombolytic Drug

ALTEPLASE (tPA) Thrombolytic Drug
Converts plasminogen to plasmin Plasmin is an enzyme that digests the fibrin matrix of clots

Uses

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Acute myocardial infarction, pulmonary embolism, and ischemic stroke

Adverse Effects Bleeding Intracranial hemorrhage

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

HEPARIN Parenteral Anticoagulant

HEPARIN Parenteral Anticoagulant
Suppresses the formation of fibrin in veins Inactivates clotting factors thrombin and Xa Anticoagulant effect develops quickly

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Uses
Prevents venous thrombosis Used for pulmonary embolism, evolving stroke, DVT Open heart surgery, MI, renal dialysis

Monitoring
Activated partial thromboplastin time (aPTT) Normal aPTT 40 seconds; therapeutic level 60 to 80 seconds

Adverse Effects
Bleeding—antidote is protamine sulfate Heparin-induced thrombocytopenia (HIT) (Decreased platelet count 100,000 leads to thrombosis) May be used during pregnancy

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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Cut here WARFARIN (COUMADIN) Oral Anticoagulant
Suppresses coagulation by antagonizing vitamin K Blocks synthesis of factors VII, IX, X, and prothrombin Effect takes a few days

WARFARIN (COUMADIN) Oral Anticoagulant

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Uses
Long-term prophylaxis of venous thrombosis Used in patients with mechanical heart valves Used in patients with atrial fibrillation

Monitoring
Prothrombin time (PT)—reported as INR Goal INR for atrial fibrillation is 2–3 Goal INR for mechanical valves is 3–4.5

Adverse Effects
Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

Hemorrhage—antidote is vitamin K Fetal harm

FERROUS SULFATE Oral Iron Preparation

FERROUS SULFATE Oral Iron Preparation
Uses
Iron deficiency anemia (microcytic hypochromic anemia)

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Adverse Effects
Nausea, heartburn, bloating, constipation, diarrhea Liquid iron preparation stains teeth Toxic to children (lethal dose is 2 to 10 grams)

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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CYANOCOBALAMIN (VITAMIN B12)

CYANOCOBALAMIN (VITAMIN B12)
Essential for synthesis of DNA Catalyzes conversion of folic acid to its active form

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Uses B12 deficiency, pernicious anemia Macrocytic normochromic anemia (megaloblastic anemia) Adverse Effects Hypokalemia

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

FOLIC ACID (FOLATE)

FOLIC ACID (FOLATE)
Essential for synthesis of DNA

Uses
Treatment of folic acid deficiency (megaloblastic anemia) Used prophylactically to prevent neural tube defects (NTDs)

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Adverse Effects
Folic acid does not correct neurologic consequences Will correct anemia, but may mask B12 deficiency Always give folic acid with B12

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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OPRELVEKIN (INTERLEUKIN-11) Thrombopoietic Growth Factor

OPRELVEKIN (INTERLEUKIN-11) Thrombopoietic Growth Factor
Stimulates production of platelets (thrombocytes)

Uses

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Used in patients undergoing chemotherapy to increase platelets

Adverse Effects Retention of sodium and water by kidney Peripheral edema Anemia, dyspnea, tachycardia

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

EPOETIN ALFA (ERYTHROPOIETIN) Hematopoietic Growth Factor

EPOETIN ALFA (ERYTHROPOIETIN) Hematopoietic Growth Factor
Stimulates production of red blood cells

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Uses Anemia of chronic renal failure Anemia due to AIDS treatment with AZT (zidovudine) Anemia caused by chemotherapy Adverse Effects Hypertension Increase in cardiovascular events Red cell aplasia

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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FILGRASTIM (NEUPOGEN) Granulocyte Colony Stimulating Factor (G-CSF)

FILGRASTIM (NEUPOGEN) Granulocyte Colony Stimulating Factor (G-CSF)
Acts on bone marrow to increase production of neutrophils

Uses

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Used in patients undergoing chemotherapy Decreases risk of infection

Adverse Effects
Bone pain, leukocytosis Elevates uric acid levels, LDH, and alkaline phosphatase Splenomegaly

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

GLIPIZIDE (GLUCOTROL) GLYBURIDE (MICRONASE) GLIMEPIRIDE (AMARYL) Oral Hypoglycemic Agents Sulfonylureas

GLIPIZIDE (GLUCOTROL) Oral Hypoglycemic Agent Sulfonylurea
Stimulates insulin release from the pancreas

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Uses
Type 2 diabetes

Adverse Effects Hypoglycemia Fetal harm

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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METFORMIN (GLUCOPHAGE) Oral Hypoglycemic Agent Biguanide
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METFORMIN (GLUCOPHAGE) Oral Hypoglycemic Agent Biguanide
Decreases blood sugar by decreasing production of glucose in the liver Enhances glucose uptake and utilization in muscle

Uses
Type 2 diabetes

Adverse Effects Decreased appetite, nausea, diarrhea, and weight loss Lactic acidosis Avoid in patients with renal or liver disease Avoid in patients with ETOH abuse, infection, or CHF Discontinue 48 hours prior to test with contrast media to avoid lactic acidosis

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

ROSIGLITAZONE (AVANDIA) PIOGLITAZONE (ACTOS) Thiazolidinediones (TZDs) “Glitazones” Insulin Sensitizers

ROSIGLITAZONE (AVANDIA) Thiazolidinedione (TZD) “Glitazone” Insulin Sensitizer
Increases insulin sensitivity

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Uses
Type 2 diabetes

Adverse Effects Fluid retention—caution in patients with CHF Hepatotoxicity—monitor ALT

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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MIGLITOL (GLYSET) ACARBOSE (PRECOSE) Alpha-Glucosidase Inhibitors Hypoglycemic Agents
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MIGLITOL (GLYSET) ACARBOSE (PRECOSE) Alpha-Glucosidase Inhibitors Hypoglycemic Agent
Delay absorption of carbohydrates Lower postprandial blood glucose levels

Uses Type 2 diabetes Adverse Effects Flatulence, cramps, abdominal distention, diarrhea Hypoglycemia, liver dysfunction

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

REPAGLINIDE (PRANDIN) NATEGLINIDE (STARLIX) Meglitinides Hypoglycemic Agents
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REPAGLINIDE (PRANDIN) NATEGLINIDE (STARLIX) Meglitinides Hypoglycemic Agents
Stimulate pancreatic insulin release

Uses
Type 2 diabetes

Adverse Effects Hypoglycemia Administer 30 minutes before meal

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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GLUCAGON

GLUCAGON
Hormone that increases plasma levels of glucose Opposite effect of insulin

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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Uses Treats hypoglycemia from insulin overdose Used only if IV glucose is not available

LEVOTHYROXINE (SYNTHROID, LEVOXYL) Thyroid Replacement Hormone Synthetic Preparation of T4
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LEVOTHYROXINE (SYNTHROID, LEVOXYL) Thyroid Replacement Hormone Synthetic Preparation of T4
Converted to T3 in the body Thyroid hormone replacement

Uses Hypothyroidism Adverse Effects
Thyrotoxicosis if dosage is excessive Tachycardia, angina, nervousness, insomnia Hyperthermia, sweating, and tremor Increases warfarin levels Takes about 1 month to reach plateau

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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PROPYLTHIOURACIL (PTU) Antithyroid Drug

PROPYLTHIOURACIL (PTU) Antithyroid Drug
Inhibits thyroid hormone synthesis

Uses

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Hyperthyroidism, Graves’ disease Thyrotoxic crisis

Adverse Effects
Agranulocytosis, hypothyroidism, rash Fetal harm

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

GLUCOCORTICOIDS

GLUCOCORTICOIDS
Suppress immune responses and inflammation Inhibit prostaglandins, leukotrienes, and histamine Suppress phagocytes and lymphocytes

Uses

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Rheumatoid arthritis, SLE, inflammatory bowel disease Bursitis, osteoarthritis, anaphylaxis, asthma Skin disorders, prevention of respiratory distress syndrome (RDS) in preterm infants Replacement therapy for patients with Addison’s disease

Adverse Effects
Adrenal insufficiency resulting from suppression of HPA axis Glucose intolerance (increases blood sugar), osteoporosis, infection Growth retardation, mood changes, cataracts, glaucoma Peptic ulcer disease, iatrogenic Cushing’s syndrome
Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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SILDENAFIL (VIAGRA) TADALAFIL (CIALIS) VARDENAFIL (LEVITRA) Erectile Dysfunction Drugs
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SILDENAFIL (VIAGRA) Erectile Dysfunction Drug
Enhances the normal erectile response to sexual stimuli by inhibiting PDE-5

Uses
Erectile dysfunction

Adverse Effects
Hypotension, priapism, headache, and flushing Visual changes Use with nitrates and alpha blockers leads to hypotension

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

PRAZOSIN (MINIPRESS) Alpha-Adrenergic Antagonist Alpha Blocker
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PRAZOSIN (MINIPRESS) Alpha-Adrenergic Antagonist Alpha Blocker
Blocks alpha1 receptors Dilates arteries and veins Relaxes smooth muscle in the bladder neck and prostatic capsule

Uses Benign prostatic hypertrophy Hypertension Adverse Effects Orthostatic hypotension, reflex tachycardia Inhibition of ejaculation Nasal congestion Use with erectile dysfunction drugs may lead to hypotension

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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LIVE VIRUS VACCINES
Varicella (Varivax) Oral Polio Vaccine (OPV) not used in the United States Measles, Mumps, and Rubella Virus Vaccine (MMR) Live Influenza Attenuated Vaccine (LIAV)

LIVE VIRUS VACCINES
Live virus vaccines are contraindicated in pregnancy Give with caution in immunocompromised patients

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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CYCLOSPORINE (SANDIMMUNE) Immunosuppressant Drug

CYCLOSPORINE (SANDIMMUNE) Immunosuppressant Drug
Suppresses production of inflammatory cells Decreases B cells and cytotoxic T cells

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Uses Organ transplant Adverse Effects Nephrotoxicity, infection, hepatotoxicity, lymphomas Hypertension, anaphylaxis, fetal harm

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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METHOTREXATE (RHEUMATREX, TREXALL) Cytotoxic Drug Immunosuppressant Disease-Modifying Antirheumatic Drug (DMARD)
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METHOTREXATE (RHEUMATREX, TREXALL) Cytotoxic Drug Immunosuppressant Disease-Modifying Antirheumatic Drug (DMARD)
Blocks conversion of folic acid to its active form Reduces joint destruction, retards disease progression Takes 3 to 5 months to see effect

Uses
Rheumatoid arthritis, non-Hodgkin’s lymphoma Lymphocytic leukemia, psoriasis

Adverse Effects
Bone marrow suppression, hepatic fibrosis GI ulceration, pneumonitis, and fetal harm
Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

DIPHENHYDRAMINE (BENADRYL) First-Generation H1 Antagonist Antihistamine
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DIPHENHYDRAMINE (BENADRYL) First-Generation H1 Antagonist Antihistamine
Blocks H1 receptors Blocks some muscarinic receptors Reduces actions of histamine Decreases flushing, itching, and secretion of mucus

Uses
Allergic rhinitis, urticaria, motion sickness, insomnia Cold symptoms, mild transfusion reactions, allergic reactions

Adverse Effects
Sedation, confusion, nausea, and dry throat
Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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LORATADINE (CLARITIN) DESLORATADINE (CLARINEX) FEXOFENADINE (ALLEGRA) CETIRIZINE (ZYRTEC)
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LORATADINE (CLARITIN) Second-Generation Nonsedating H1 Antagonist (Antihistamine)
Blocks H1 receptors Reduces actions of histamine Decreases flushing, itching, secretion of mucus Does not cross blood-brain barrier to cause sedation

Second-Generation Nonsedating H1 Antagonists (Antihistamines)

Uses Allergic rhinitis, urticaria, and mild transfusion reactions Adverse Effects
Decrease dose if hepatic or renal impairment occurs Cetirizine (Zyrtec) may cause mild sedation in some patients

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

ASPIRIN Antiplatelet Drug Cyclooxygenase (COX) Inhibitor First-Generation NSAID
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ASPIRIN Antiplatelet Drug Cyclooxygenase (COX) Inhibitor First-Generation NSAID
Suppresses platelet aggregation by inhibiting COX-1 and COX-2 Decreases prostaglandin synthesis Reduces inflammation, pain, and fever

Uses Pain, fever, inflammation Prevention of thrombus in arteries Prevents MI and stroke Adverse Effects Bleeding, gastric ulceration, renal impairment Not used in children because of Reye’s syndrome Fetal harm, salicylism Hypersensitivity in patients with allergies

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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IBUPROFEN (ADVIL, MOTRIN) First-Generation NSAID

IBUPROFEN (ADVIL, MOTRIN) First-Generation NSAID
Inhibits cyclooxygenase (COX)-1 and COX-2 Inhibits prostaglandin synthesis Has antiinflammatory, analgesic, and antipyretic actions

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Uses Dysmenorrhea, arthritis, pain, and fever Adverse Effects
Bleeding, gastric ulceration, renal impairment Cross-hypersensitivity with aspirin May precipitate Reye’s syndrome, fetal harm

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

CELECOXIB (CELEBREX) Second-Generation NSAID COX-2 Inhibitor
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CELECOXIB (CELEBREX) Second-Generation NSAID COX-2 Inhibitor
Selective inhibition of COX-2, decreases prostaglandin synthesis (pain and inflammation reduced) Spares COX-1 inhibition Minimal gastric, renal, and platelet effect

Uses
Osteoarthritis, rheumatoid arthritis, dysmenorrhea Acute pain

Adverse Effects
Dyspepsia, mild renal impairment Not used in patients with sulfonamide allergy Premature closure of ductus arteriosus
Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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ACETAMINOPHEN (TYLENOL) Analgesic Antipyretic
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ACETAMINOPHEN (TYLENOL) Analgesic Antipyretic
Decreases prostaglandin synthesis in the CNS Devoid of antiinflammatory properties

Uses
Pain and fever Preferred in children No GI injury, no effect on platelets or kidneys

Adverse Effects
Toxic metabolite builds up in ETOH abusers Hepatic necrosis can occur Acetylcysteine (Mucomyst) given for overdose
Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

FLUTICASONE PROPIONATE (FLOVENT) Inhaled Corticosteroid (ICS)

FLUTICASONE PROPIONATE (FLOVENT) Inhaled Corticosteroid (ICS)
Suppresses inflammation Decreases leukotrienes, histamine, and prostaglandins Decreases eosinophils and leukocytes Reduces edema of airway and mucous production Reduces bronchial hyperactivity Increases number and responsiveness of beta2 receptors

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Uses Asthma Adverse Effects Oropharyngeal candidiasis—rinse mouth after use Minimal adrenal suppression and bone loss Slows growth but does not reduce adult height Slight increased risk of cataracts and glaucoma

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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SALMETEROL (SEREVENT) Long-Acting Inhaled Beta2-Adrenergic Agonist

SALMETEROL (SEREVENT) Long-Acting Inhaled Beta2-Adrenergic Agonist
Activates beta2 receptors in the lung Promotes bronchodilation Suppresses histamine release in the lung Increases ciliary motility

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Uses Asthma Adverse Effects Effect is delayed by 20 to 30 minutes Not to be used as a rescue inhaler in an emergency Tachycardia, angina, tremor, and leg cramps

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

MONTELUKAST (SINGULAIR) Leukotriene Modifier

MONTELUKAST (SINGULAIR) Leukotriene Modifier
Blocks leukotriene receptors Decreases inflammation, bronchoconstriction, and edema Decreases mucous secretion Decreases eosinophils and other inflammatory cells Reduces dosage of inhaled corticosteroid (ICS)

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Uses Asthma and allergic rhinitis Adverse Effects GI upset Effect is delayed

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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THEOPHYLLINE Methylxanthine Bronchodilator
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THEOPHYLLINE Methylxanthine Bronchodilator
Produces bronchodilation by relaxing bronchi

Uses Asthma (beta2 agonists and corticosteroids preferred) Adverse Effects Narrow therapeutic range (5 to 10 mcg/mL) Dysrhythmias, ventricular fibrillation Convulsions, cardiorespiratory collapse, and death

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

ALBUTEROL (PROVENTIL, VENTOLIN, ACCUNEB) Beta2-Adrenergic Agonist Bronchodilator
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ALBUTEROL (PROVENTIL, VENTOLIN, ACCUNEB) Beta2-Adrenergic Agonist Bronchodilator
Stimulates beta2 receptors in the lung Bronchodilation Rapid onset of action for rescue breathing

Uses Asthma Adverse Effects Hyperglycemia, tachycardia, tremor

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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RANITIDINE (ZANTAC) CIMETIDINE (TAGAMET) FAMOTIDINE (PEPCID) NIZATIDINE (AXID)
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RANITIDINE (ZANTAC) Histamine2-Receptor Antagonist
Blocks H2 receptors on parietal cells of the stomach Reduces volume of gastric juice and hydrogen ion content

Histamine2-Receptor Antagonists

Uses
Gastric and duodenal ulcers Gastroesophageal reflux disease (GERD), dyspepsia Treatment of Zollinger-Ellison syndrome

Adverse Effects Significant side effects are uncommon

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

OMEPRAZOLE (PRILOSEC) LANSOPRAZOLE (PREVACID) RABEPRAZOLE (ACIPHEX) PANTOPRAZOLE (PROTONIX) ESOMEPRAZOLE (NEXIUM) Proton Pump Inhibitors (PPIs)
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OMEPRAZOLE (PRILOSEC) Proton Pump Inhibitor (PPI)
Inhibits the enzyme that generates acid production

Uses Duodenal and gastric ulcers, GERD, dyspepsia Zollinger-Ellison syndrome Adverse Effects Headache, diarrhea, nausea, and vomiting

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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SUCRALFATE (CARAFATE) Antiulcer drug

SUCRALFATE (CARAFATE) Antiulcer drug
Creates a protective barrier against acid and pepsin Sticky gel adheres to ulcer crater

Uses

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Duodenal and gastric ulcers

Adverse Effects
May impede the absorption of some drugs Separate at least 2 hours from other drugs

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

METOCLOPRAMIDE (REGLAN) Prokinetic Drug

METOCLOPRAMIDE (REGLAN) Prokinetic Drug
Reduces emesis by blocking receptors in the chemoreceptor trigger zone (CTZ) Increases upper GI motility by enhancing the actions of ACh

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Uses
Suppresses nausea caused by chemotherapy Suppresses postoperative emesis and GERD

Adverse Effects
Sedation and diarrhea Extrapyramidal reactions, especially in children

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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SULFASALAZINE (AZULFIDINE) Aminosalicylate

SULFASALAZINE (AZULFIDINE) Aminosalicylate
Reduces inflammation

Uses

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Inflammatory bowel disease Crohn’s disease and ulcerative colitis

Adverse Effects
Nausea, fever, rash, and arthralgias Agranulocytosis, hemolytic anemia, and macrocytic anemia

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

ONDANSETRON (ZOFRAN) Antiemetic Drug Serotonin-Receptor Antagonist
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ONDANSETRON (ZOFRAN) Antiemetic Drug Serotonin-Receptor Antagonist
Suppresses emesis by blocking 5-HT3 receptors in the chemoreceptor trigger zone (CTZ)

Uses Decreases nausea and vomiting due to: Chemotherapy, radiation therapy, and anesthesia (postoperatively) Adverse Effects Headache, nausea, and dizziness

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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PROCHLORPERAZINE (COMPAZINE) PROMETHAZINE (PHENERGAN) Antiemetic Drugs Dopamine Antagonists
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PROCHLORPERAZINE (COMPAZINE) Antiemetic Drug Dopamine Antagonist
Suppresses emesis by blocking dopamine2 receptors in the CTZ

Uses Nausea and vomiting Used after surgery, cancer chemotherapy, or other conditions Adverse Effects Extrapyramidal reactions, anticholinergic effects Hypotension and sedation

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

HYDROXYZINE (VISTARIL, ATARAX) Antiemetic Drug Anticholinergic-Antihistamine
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HYDROXYZINE (VISTARIL, ATARAX) Antiemetic Drug Anticholinergic-Antihistamine
Blocks histaminergic and cholinergic receptors

Uses
Nausea

Adverse Effects
Sedation, blurry vision, urinary retention, dry mouth

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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PENICILLIN G (BENZYLPENICILLIN) Narrow-Spectrum Penicillin

PENICILLIN G (BENZYLPENICILLIN) Narrow-Spectrum Penicillin
Weakens the bacterial cell wall

Uses

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Treats Streptococcus, Neisseria, anaerobes, and others Drug of choice for syphilis

Adverse Effects
Allergic reaction, pain at site of injection Neurotoxicities

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

NAFCILLIN (UNIPEN) Penicillinase-Resistant Penicillin (Antistaphylococcal Penicillin)
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NAFCILLIN (UNIPEN) Penicillinase-Resistant Penicillin (Antistaphylococcal Penicillin)
Weakens the cell wall

Uses
Treats infections caused by Staphylococcus aureus

Adverse Effects
Allergic reaction, GI effects Thrombophlebitis, hypokalemia

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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AMOXICILLIN (AMOXIL) Broad-Spectrum Penicillin (Aminopenicillin)

AMOXICILLIN (AMOXIL) Broad-Spectrum Penicillin (Aminopenicillin)
Weakens the bacterial cell wall

Uses

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Treats infections caused by Haemophilus influenzae, Escherichia coli, Proteus mirabilis, enterococci Neisseria gonorrhoeae

Adverse Effects Diarrhea

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

CEFAZOLIN (KEFZOL, ANCEF) First-Generation Cephalosporin Beta-Lactam Antibiotic
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CEFAZOLIN (KEFZOL, ANCEF) First-Generation Cephalosporin Beta-Lactam Antibiotic
Weakens the bacterial cell wall

Uses
Gram-positive infections Surgical prophylaxis

Adverse Effects Allergic reaction Bleeding tendencies Thrombophlebitis Antibiotic-associated pseudomembranous colitis (AAPMC)

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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CEFUROXIME (CEFTIN) Second-Generation Cephalosporin Beta-Lactam Antibiotic
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CEFUROXIME (CEFTIN) Second-Generation Cephalosporin Beta-Lactam Antibiotic
Weakens the bacterial cell wall

Uses Upper respiratory tract infections Acute otitis media (AOM) and sinusitis Adverse Effects Allergic reaction Bleeding tendencies Thrombophlebitis Antibiotic-associated pseudomembranous colitis (AAPMC)

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

CEFTRIAXONE (ROCEPHIN) Third-Generation Cephalosporin Beta-Lactam Antibiotic
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CEFTRIAXONE (ROCEPHIN) Third-Generation Cephalosporin Beta-Lactam Antibiotic
Weakens the bacterial cell wall

Uses
Active against gram-negative organisms

Adverse Effects Allergic reaction Bleeding tendencies Thrombophlebitis Antibiotic-associated pseudomembranous colitis (AAPMC)

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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VANCOMYCIN (VANCOCIN) Antibiotic

VANCOMYCIN (VANCOCIN) Antibiotic
Inhibits bacterial cell wall synthesis

Uses

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Active against gram-positive bacteria Serious infections, such as methicillin-resistant Staphylococcus aureus (MRSA) Antibiotic-associated pseudomembranous colitis (AAPMC) Used for patients allergic to penicillin

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

Adverse Effects Ototoxicity Rapid infusion can lead to “red man syndrome” (flushing, tachycardia, and hypotension) Infuse over 60 minutes or more Thrombophlebitis

TETRACYCLINE DOXYCYCLINE MINOCYCLINE Broad-Spectrum Antibiotics
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TETRACYCLINE Broad-Spectrum Antibiotic
Suppresses bacterial growth by inhibiting protein synthesis

Uses Rocky Mountain spotted fever, typhus Chlamydia trachomatis, Mycoplasma pneumonia Helicobacter pylori, anthrax, and Lyme disease Acne, peptic ulcer disease, periodontal disease Adverse Effects
GI irritation, suprainfection (AAPMC) Discoloration of teeth (avoid in children 8 years old) Hepatotoxicity, exacerbation of renal impairment Photosensitivity, vestibular toxicity

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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ERYTHROMYCIN CLARITHROMYCIN (BIAXIN) AZITHROMYCIN (ZITHROMAX) DIRITHROMYCIN (DYNABAC) TELITHROMYCIN (KETEK) Macrolide Antibiotics Broad-Spectrum Antibiotics
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ERYTHROMYCIN Macrolide Antibiotic Broad-Spectrum Antibiotic
Inhibits bacterial cell wall synthesis

Uses Active against most gram-positive and some gram-negative organisms Treats atypicals such as Legionella pneumonia, pertussis, diphtheria, and pneumonia caused by Mycoplasma pneumoniae Can be used as an alternative to PCN in allergic individuals Adverse Effects
GI effects, liver injury Inhibitor of cytochrome P450 Increases levels of theophylline, carbamazepine, and some statins

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

CLINDAMYCIN (CLEOCIN) Antibiotic

CLINDAMYCIN (CLEOCIN) Antibiotic
Inhibits bacterial protein synthesis

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Uses Active against most anaerobic bacteria outside the CNS Bacteroides fragilis, Fusobacterium, Clostridium perfringens Adverse Effects Antibiotic-associated pseudomembranous colitis (AAPMC) Diarrhea

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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GENTAMICIN (GARAMYCIN) AMIKACIN (AMIKIN) TOBRAMYCIN (NEBCIN) Aminoglycoside Antibiotics Narrow-Spectrum Antibiotics

GENTAMICIN (GARAMYCIN) Aminoglycoside Antibiotic Narrow-Spectrum Antibiotic
Disrupts bacterial protein synthesis

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Uses Effective against aerobic gram-negative bacilli Adverse Effects Nephrotoxicity (renal dosing required to avoid toxic drug levels) Ototoxicity (requires peak and trough level monitoring) Intensifies neuromuscular blockade, leading to respiratory arrest Incompatible with PCN

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

TRIMETHOPRIM/SULFAMETHOXAZOLE (TMP-SMZ-BACTRIM) Antibiotic
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TRIMETHOPRIM/SULFAMETHOXAZOLE (TMP-SMZ-BACTRIM) Antibiotic
Combination antibiotic that inhibits bacterial synthesis of folic acid

Uses
Urinary tract infections Pneumonia caused by Pneumocystis carinii

Adverse Effects
Nausea, vomiting, rash, blood dyscrasias Hypersensitivity reactions (Stevens-Johnson syndrome) Not for use in patients with sulfa allergies Avoid use in pregnant women near term Avoid use in infants under the age of 2 months

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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CIPROFLOXACIN (CIPRO) MOXIFLOXACIN (AVELOX) GATIFLOXACIN (TEQUIN) LEVOFLOXACIN (LEVAQUIN)
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CIPROFLOXACIN (CIPRO) Fluoroquinolone Antibiotic
Inhibits bacterial DNA

Uses

Fluoroquinolone Antibiotics

Infections of the urinary, respiratory, and GI tracts; bones; joints; skin; and soft tissues

Adverse Effects
GI upset, CNS effects (dizziness, headache, restlessness) Achilles tendon rupture Do not take with milk products Elevates levels of warfarin Not recommended for children under 18 years old Avoid in pregnancy

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

METRONIDAZOLE (FLAGYL) Antibacterial Drug

METRONIDAZOLE (FLAGYL) Antibacterial Drug
Causes cell death by damaging bacterial DNA

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Uses Protozoal infection Infections caused by obligate anaerobic bacteria Bacteroides, Clostridium difficile, Helicobacter pylori, Trichomonas vaginalis, giardiasis Used as prophylaxis in colorectal or abdominal surgery Adverse Effects
Nausea, headache, dry mouth, metallic taste Dark discoloration of urine Disulfiram-like effect when used with alcohol Increases warfarin levels

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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KETOCONAZOLE (NIZORAL) FLUCONAZOLE (DIFLUCAN) ITRACONAZOLE (SPORANOX) MICONAZOLE (MONISTAT) CLOTRIMAZOLE Antifungal Agents
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KETOCONAZOLE (NIZORAL) Antifungal Agent
Causes bacterial cell wall to leak

Uses
Systemic and superficial mycoses (fungi)

Adverse Effects Hepatotoxicity (monitor liver function tests [LFTs]) Decreases sex hormones Don’t give with PPIs Inhibits hepatic drug-metabolizing enzymes Increases levels of warfarin, phenytoin, and some statins

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

GRISEOFULVIN Antifungal Agent

GRISEOFULVIN Antifungal Agent
Inhibits fungal mitosis

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Uses Superficial mycoses (fungi) Dermatophytic infections of the skin, hair, and nails Not active against Candida species or systemic mycoses May take 3 to 8 weeks to respond Adverse Effects
May decrease the effects of warfarin

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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ACYCLOVIR (ZOVIRAX) VALACYCLOVIR (VALTREX) FAMCICLOVIR (FAMVIR) Antiviral Agents
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ACYCLOVIR (ZOVIRAX) Antiviral Agent
Suppresses synthesis of viral DNA

Uses
Herpesvirus, varicella-zoster virus, cytomegalovirus (CMV)

Adverse Effects IV administration can lead to phlebitis and nephrotoxicity Infuse slowly over 1 hour and maintain hydration Oral therapy may lead to nausea, vomiting, diarrhea Headache and vertigo

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

INTERFERON ALPHA Antiviral Agent

INTERFERON ALPHA Antiviral Agent
Decreases viral replication

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Uses Hepatitis B and C Adverse Effects Flulike syndrome Depression Fatigue, hair loss, thyroid damage, heart damage Bone marrow suppression

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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RIBAVIRIN (REBETOL) Antiviral Agent

RIBAVIRIN (REBETOL) Antiviral Agent
Uses Used with interferon for treatment of hepatitis C

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Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

Adverse Effects Hemolytic anemia Fetal harm (Category X) Use second reliable form of birth control during treatment and 6 months after treatment

NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs) Zidovudine (Retrovir) Lamivudine (Epivir) Zalcitabine (Hivid) Antiretroviral Drugs

NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs) Antiretroviral Drugs
Suppress the synthesis of viral DNA by blocking transcriptase

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Uses
HIV infection

Adverse Effects
Anemia, neutropenia, lactic acidosis

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)
Delavirdine (Rescriptor) Efavirenz (Sustiva) Nevirapine (Viramune)

NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs) Antiretroviral Drugs
Inhibit reverse transcriptase by binding to it

Antiretroviral Drugs

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Uses HIV infection Adverse Effects Rash, Stevens-Johnson syndrome, erythema multiforme Hepatotoxicity

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

PROTEASE INHIBITORS
Nelfinavir (Viracept) Ritonavir (Norvir) Saquinavir (Invirase)

PROTEASE INHIBITORS Antiretroviral Drugs
Inhibit the enzyme protease, needed for HIV to mature

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Antiretroviral Drugs

Uses HIV Adverse Effects
Hyperglycemia, diabetes, fat redistribution, hyperlipidemia Increased bleeding in hemophiliac patients Reduced bone mineral density Elevation of serum transaminases Can increase or decrease levels of other drugs

Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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