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Drug Receptor Types

Functions of Peripheral Adrenergic Receptor Subtypes Functions of Peripheral Cholinergic Receptor Subtypes
Receptor Receptor
Subtype Location Response to Receptor Activation Subtype Location Response to Receptor Activation
Alpha1 Eye Mydriasis—wide eyed with fear Nicotinicn All autonomic nervous system Stimulation of parasympathetic and
Arterioles (skin, viscera, mucous Constriction ganglia and the adrenal medulla sympathetic postganglionic nerves and
membranes) release of epinephrine from the adrenal
Veins Constriction medulla

Fold here
Sex organs, male Ejaculation Nicotinicm Neuromuscular junction Contraction of skeletal muscle
Bladder neck and prostatic capsule Contraction Muscarinic All parasympathetic target organs:
Alpha2 Presynaptic nerve terminals Inhibition of transmitter release—decreases Eye Miosis
sympathetic nervous system (SNS) out- Heart Decreased rate
flow to the blood vessels and heart Lung Constriction of bronchi
Beta1 Heart Increased rate, force of contraction, and AV Promotion of secretions
conduction velocity
Bladder Voiding
Kidney Renin release—RAS
GI tract Salivation
Beta2 Arterioles (heart, lung, and Dilation
skeletal mucle) Increases gastric secretions, intestinal
Bronchi Dilation tone, and motility
Uterus Relaxation Defecation
Liver Glycogenolysis Sweat glands Generalized sweating
Skeletal muscle Enhanced contraction, glycogenolysis Sex organs Erection
Dopamine Kidney Dilation of kidney vasculature Blood vessels Vasodilation

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Drug Endings Drug Endings—cont’d


Drug Endings Drug Classification Drug Example Drug Endings Drug Classification Drug Example
-zosin Alpha-adrenergic blocker prazosin -terol Bronchodilator albuterol
-olol, -lol Beta-adrenergic blocker metoprolol -tidine Histamine2 blocker–acid reducer cimetidine
Fold here

-zepam, -zolam Benzodiazepine (BZD) diazepam, alprazolam -prazole Protein pump inhibitor–acid reducer omeprazole
-pril Angiotensin-converting enzyme (ACE) inhibitor lisinopril -cillin Penicillin antibiotic amoxicillin
-artan Angiotensin-receptor blocker (ARB) candesartan -cef, -ceph Cephalosporin antibiotic cefazolin
-dipine Calcium channel blocker amlodipine -cycline Tetracycline antibiotic tetracycline
-statin Lipid-lowering drug atorvastatin -floxacin Fluoroquinolone antibiotic levofloxacin
-ase, -plase Thrombolytic alteplase -thromycin Macrolide antibiotic azithromycin
-parin Anticoagulant enoxaparin -micin, -mycin Aminoglycoside antibiotic gentamycin
-sone Corticosteroid prednisone -azole Antifungal itraconazole
-dronate Bisphosphonate for osteoporosis alendronate
Continued

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


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

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

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

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ATROPINE ATROPINE
Muscarinic Antagonist (Anticholinergic)
Muscarinic Antagonist (Anticholinergic)
Blocks muscarinic receptors
Increases heart rate
Decreases salivary, bronchial, sweat, and acid-secreting cell secretions
Relaxes bronchial smooth muscles
Fold here

Decreases bladder tone and GI motility


Dilates pupils (mydriasis)
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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Blurry vision, urinary retention, dry mouth, constipation, tachycardia
Increases intraocular pressure
NEOSTIGMINE (PROSTIGMINE) NEOSTIGMINE (PROSTIGMINE)
Reversible Cholinesterase Inhibitor
Reversible Cholinesterase Inhibitor
Prevents the degradation of acetylcholine (ACh)
Enhances the effect of ACh to stimulate skeletal muscle
Uses

Fold here
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

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

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SUCCINYLCHOLINE SUCCINYLCHOLINE
Depolarizing Neuromuscular Blocker
Depolarizing Neuromuscular Blocker
Causes paralysis of muscle by preventing repolarization
Uses
Muscle relaxation during endotracheal intubation
Fold here

Used for short operative procedures


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

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


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

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

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

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EPINEPHRINE EPINEPHRINE
Adrenergic Agonist (Catecholamine)
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
Fold here

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
Adverse Effects
Hypertension, tachycardia, and dysrhythmias
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Angina, necrosis following extravasation
Hyperglycemia in diabetic patients
PROPRANOLOL (INDERAL) PROPRANOLOL (INDERAL)
Adrenergic Antagonist
Adrenergic Antagonist Noncardioselective Beta Blocker
Noncardioselective Beta Blocker
Blocks beta1 and beta2 receptors
Reduces heart rate, decreases force of ventricular contraction
Decreases conduction through AV node, decreases cardiac output

Fold here
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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Not used in patients with asthma or diabetes

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METOPROLOL (LOPRESSOR, TOPROL XL) METOPROLOL (LOPRESSOR, TOPROL XL)


Adrenergic Antagonist
Adrenergic Antagonist Cardioselective Beta Blocker
Cardioselective Beta Blocker
Blocks cardiac beta1 receptors
Reduces heart rate, decreases force of ventricular contraction
Decreases conduction through AV node, decreases cardiac output
Fold here

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
Bradycardia, reduction of cardiac output, AV heart block
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Rebound cardiac excitation following abrupt withdrawal
PRAZOSIN (MINIPRESS) PRAZOSIN (MINIPRESS)
Adrenergic Antagonist
Adrenergic Antagonist Alpha blocker
Alpha Blocker
Blocks alpha1 receptors
Dilates arteries and veins
Relaxes smooth muscle in the bladder neck and prostatic capsule

Fold here
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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. lead to hypotension

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CLONIDINE (CATAPRES) CLONIDINE (CATAPRES)


Centrally Acting Alpha2 Agonist
Centrally Acting Alpha2 Agonist Antihypertensive Drug
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
Fold here

Net effect of cardiac suppression and vasodilation is decreased


blood pressure
Uses
Hypertension
Adverse Effects
Hypotension
Bradycardia, decrease in cardiac output
Drowsiness, dry mouth
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Rebound hypertension in response to abrupt withdrawal
Fetal harm
LEVODOPA/CARBIDOPA (SINEMET) LEVODOPA/CARBIDOPA (SINEMET)
Dopaminergic Agent
Dopaminergic Agent
Levodopa increases synthesis of dopamine in the striatum
Carbidopa enhances the effect of levodopa
Uses

Fold here
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

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

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DONEPEZIL (ARICEPT) DONEPEZIL (ARICEPT)


Cholinesterase Inhibitor
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
Fold here

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

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


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

Fold here
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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Withdraw over a period of 6 to 8 weeks to avoid seizures

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VALPROIC ACID (DEPAKOTE) VALPROIC ACID (DEPAKOTE)


Antiepileptic Drug (AED)
Antiepileptic Drug (AED)
Blocks sodium channels to suppress neurons
Suppresses calcium influx
Fold here Increases inhibitory influence of gamma-aminobutyric acid (GABA)
Uses
Epilepsy, bipolar disorder, migraine headaches
Adverse Effects
Nausea, vomiting, indigestion
Hepatotoxicity, pancreatitis, fetal harm
Weight gain, rash, hair loss, tremor
Blood dyscrasias

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


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

Fold here
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)

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

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NALOXONE (NARCAN) NALOXONE (NARCAN)


Opioid Antagonist
Opioid Antagonist
Reverses the effects of opioids
Uses
Opioid overdose
Fold here

Reversal of excessive respiratory depression


Adverse Effects
Minimal

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


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

Fold here
Uses
Migraine headache
Adverse Effects
Chest pressure, coronary vasospasm
Fetal harm

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

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CONVENTIONAL ANTIPSYCHOTICS CONVENTIONAL ANTIPSYCHOTICS


(NEUROLEPTICS) (NEUROLEPTICS)
Chlorpromazine (Thorazine) Relieve positive symptoms of schizophrenia
Thioridazine (Mellaril) Block receptors for dopamine, acetylcholine (ACh), histamine, and
Haloperidol (Haldol) norepinephrine (NE)
Uses
Fold here

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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc.
ATYPICAL ANTIPSYCHOTICS ATYPICAL ANTIPSYCHOTICS
Clozapine (Clozaril) Relieve positive and negative signs and symptoms of schizophrenia
Risperidone (Risperdal) Block receptors for serotonin, dopamine, ACh, histamine, and NE
Olanzapine (Zyprexa) Clinically superior to conventional antipsychotics
Quetiapine (Seroquel)
Ziprasidone (Geodon) Uses
Aripiprazole (Abilify) Schizophrenia

Fold here
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

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

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SELECTIVE SEROTONIN REUPTAKE SELECTIVE SEROTONIN REUPTAKE


INHIBITORS (SSRIs) INHIBITORS (SSRIs)
Fluoxetine (Prozac) Antidepressants
Paroxetine (Paxil)
Sertraline (Zoloft) Inhibit serotonin reuptake (more serotonin is available at the synapse)
Citalopram (Celexa) Uses
Escitalopram (Lexapro)
Fold here

Major depression, OCD


Panic disorder, PTSD, PMDD
Antidepressants
Adverse Effects
Sexual dysfunction, nausea, headache, insomnia
Weight gain, serotonin syndrome
Withdrawal syndrome

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


TRICYCLIC ANTIDEPRESSANTS (TCAs) TRICYCLIC ANTIDEPRESSANTS (TCAs)
Amitriptyline (Elavil) Antidepressants
Clomipramine (Anafranil)
Desipramine (Norpramin) Inhibit reuptake of NE and serotonin (more serotonin and NE available at
Doxepin (Sinequan) the synapse)
Uses

Fold here
Antidepressants 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

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

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MONOAMINE OXIDASE INHIBITORS (MAOIs) MONOAMINE OXIDASE INHIBITORS (MAOIs)


Antidepressants
Antidepressants
Increase NE and serotonin by blocking enzyme that inactivates them
Uses
Depression
Fold here

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

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


LITHIUM LITHIUM
Mood-Stabilizing Drug
Mood-Stabilizing Drug
Mechanism unclear, may alter ions and neurotransmitters
Uses
Stabilizes mood in patients with bipolar disorder

Fold here
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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Pregnancy Risk Category D
Drug interactions occur with diuretics, NSAIDs, and anticholinergics

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VALPROIC ACID (DEPAKOTE) VALPROIC ACID (DEPAKOTE)


Mood-Stabilizing Anticonvulsant
Mood-Stabilizing Anticonvulsant
Suppresses mania and stabilizes mood
Uses
Mood stabilizer for patients with bipolar disorder
Fold here

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

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


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

Fold here
Adverse Effects
Headache, dizziness, double vision
Life-threatening rashes include Stevens-Johnson syndrome and
epidermal necrolysis

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

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BENZODIAZEPINES (BZDs) BENZODIAZEPINES (BZDs)


Alprazolam (Xanax) Sedative Hypnotic Drugs
Diazepam (Valium)
Flurazepam (Dalmane) Depress central nervous system function
Lorazepam (Ativan) Reduce anxiety, promote sleep
Midazolam (Versed) Potentiate the actions of GABA (an inhibitory neurotransmitter)
Temazepam (Restoril)
Fold here
Uses
Anxiety, insomnia, seizure disorder, induction of anesthesia
Sedative-Hypnotic Drugs 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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Reversal agent is flumazenil (Romazicon)
ZOLPIDEM (AMBIEN) ZOLPIDEM (AMBIEN)
ZALEPLON (SONATA) Sedative-Hypnotics
BZD-like Drugs
Sedative-Hypnotics
Potentiate the actions of GABA (an inhibitory neurotransmitter)
BZD-like Drugs
Uses

Fold here
Short-term management of insomnia
Adverse Effects
Daytime drowsiness, dizziness
Do not use with alcohol or other CNS depressants

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

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BARBITURATES BARBITURATES
Thiopental (Pentothal)
CNS Depressants
Secobarbital (Seconal)
Phenobarbital Potentiate the actions of GABA (an inhibitory neurotransmitter)
Uses
CNS Depressants Insomnia
Fold here

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

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


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

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

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ATOMOXETINE (STRATTERA) ATOMOXETINE (STRATTERA)


Nonstimulant Drug for ADHD
Nonstimulant Drug for ADHD
Selective inhibitor of NE reuptake
Causes NE to accumulate at synapses
Uses
Fold here

ADHD in children and adults


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

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


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

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

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

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DISULFIRAM (ANTABUSE) DISULFIRAM (ANTABUSE)


Aversion Therapy for Alcoholism
Aversion Therapy for Alcoholism
Disrupts alcohol metabolism by blocking enzyme
Aldehyde accumulates and produces unpleasant effects
Uses
Fold here

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

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


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

Fold here
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)

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

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HYDROCHLOROTHIAZIDE (HCTZ) HYDROCHLOROTHIAZIDE (HCTZ)


Thiazide Diuretic
Thiazide Diuretic
Blocks reabsorption of sodium and chloride in the early segment of the
distal convoluting tubule to promote urination
Uses
Fold here

Treatment of hypertension
Mobilization of edema with mild heart failure, hepatic or renal disease
Adverse Effects
Hyponatremia, hypochloremia, dehydration
Hypokalemia and hypotension

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


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

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

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

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ENALAPRIL (VASOTEC) ENALAPRIL (VASOTEC)


Benazepril (Lotensin) Angiotensin-Converting Enzyme (ACE) Inhibitor
Fosinopril (Monopril)
Lisinopril (Prinivil and Zestril) Inhibits ACE, reducing levels of angiotensin II
Moexipril (Univasc) Dilates arterioles and veins to reduce BP
Perindopril (Aceon) Reduces blood volume
Quinapril (Accupril)
Fold here
Uses
Ramipril (Altace)
Trandolapril (Mavik) Hypertension, heart failure, MI, diabetic nephropathy
Prevention of MI, stroke, and death

Angiotensin-Converting Enzyme (ACE) Inhibitors Adverse Effects


Hypotension, cough, hyperkalemia
Renal failure in patients with renal artery stenosis
Fetal injury
Angioedema

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


LOSARTAN (COZAAR) LOSARTAN (COZAAR)
Candesartan (Atacand) Angiotensin II-Receptor Blocker (ARB)
Eprosartan (Teveten)
Olmesartan (Benicar) Blocks the actions of angiotensin II
Telmisartan (Micardis) Dilates arterioles and veins to reduce BP
Valsartan (Diovan) Reduces blood volume

Fold here
Uses
Angiotensin II-Receptor Blockers (ARBs) Hypertension, heart failure, MI, and diabetic nephropathy
Prevention of MI, stroke, and death
Adverse Effects
Renal failure in patients with renal artery stenosis
Hypotension
Angioedema
Fetal injury
Does not cause cough or hyperkalemia
Copyright © 2007 by Saunders, an imprint of Elsevier Inc.

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VERAPAMIL (CALAN) VERAPAMIL (CALAN)


DILTIAZEM (CARDIZEM) DILTIAZEM (CARDIZEM)
Calcium Channel Blockers (CCBs)
Calcium Channel Blockers (CCBs) Nondihydropyridines
Nondihydropyridines
Block calcium channels in the heart and blood vessels
Reduce BP by blocking calcium channels in the arterioles
Fold here

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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc.
AMLODIPINE (NORVASC) AMLODIPINE (NORVASC)
Calcium Channel Blocker
Calcium Channel Blocker
Dihydropyridine Dihydropyridine
Blocks calcium channels in the blood vessels
Vasodilation in peripheral arterioles lowers blood pressure

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

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

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DIGOXIN (LANOXIN) DIGOXIN (LANOXIN)


Cardiac Glycoside
Positive Inotropic Agent
Cardiac Glycoside Drug for Heart Failure
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
Fold here

↓K → ↑ Na, K-ATPase inhibition → digoxin toxicity


Changes electrical activity of the heart and slows heart rate

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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Inject slowly over 5 minutes
Give Digibind for digoxin overdose
AMIODARONE (CORDARONE) AMIODARONE (CORDARONE)
Antidysrhythmic
Antidysrhythmic Class III Potassium Channel Blocker
Class III Potassium Channel Blocker Delays repolarization
Reduces automaticity in the SA node, reduces contractility
Decreases conduction velocity in the AV node, ventricles, and

Fold here
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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Hepatitis, thyroid dysfunction
Toxicities in pregnancy
Grapefruit juice increases levels to toxicity

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VERAPAMIL (CALAN) VERAPAMIL (CALAN)


DILTIAZEM (CARDIZEM) DILTIAZEM (CARDIZEM)
Antidysrhythmics
Antidysrhythmics Class IV Calcium Channel Blockers
Class IV Calcium Channel Blockers
Block calcium channels in the heart
Slow SA node automaticity, delay AV nodal conduction
Fold here

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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Grapefruit juice increases levels to toxicity
PROCAINAMIDE (PRONESTYL) PROCAINAMIDE (PRONESTYL)
Antidysrhythmic
Antidysrhythmic Class IA Sodium Channel Blocker
Class IA Sodium Channel Blocker
Blocks cardiac sodium channels
Slows conduction in the atria, ventricles, and His-Purkinje system
Delays depolarization

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

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

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LIDOCAINE (XYLOCAINE) LIDOCAINE (XYLOCAINE)


Antidysrhythmic
Antidysrhythmic Class IB Sodium Channel Blocker
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
Fold here

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

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


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

Fold here
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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Bronchospasm in patients with asthma

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ATORVASTATIN (LIPITOR) ATORVASTATIN (LIPITOR)


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

Lipid-Lowering Drugs Uses


HMG-CoA Reductase Inhibitors (Statins) 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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Cyclosporine, macrolide antibiotics, azole antifungals, and HIV protease
inhibitors raise some statins to toxic levels
NICOTINIC ACID (NIACIN) NICOTINIC ACID (NIACIN)
Lipid-Lowering Agent
Lipid-Lowering Agent
Reduces LDL and triglycerides
Increases HDL
Uses

Fold here
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) CHOLESTYRAMINE (QUESTRAN)


COLESEVELAM (WELCHOL) Bile-Acid Sequestrant
Forms insoluble complex with bile acids
Bile-Acid Sequestrants Increases LDL receptors
Fold here 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) GEMFIBROZIL (LOPID)
FENOFIBRATE (TRICOR) Fibric Acid Derivative (Fibrate)
Decreases triglycerides by lowering VLDL
Fibric Acid Derivatives (Fibrates) Raises HDL levels
Uses

Fold here
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) EZETIMIBE (ZETIA)


Cholesterol-Lowering Drug
Cholesterol-Lowering Drug
Blocks cholesterol absorption in the small intestine
Uses
Hypercholesterolemia
Fold here

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

Fold here
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) CLOPIDOGREL (PLAVIX)


Adenosine Diphosphate–Receptor Antagonist
Adenosine Diphosphate–Receptor Antagonist ADP Receptor Blocker
ADP Receptor Blocker Antiplatelet Drug
Antiplatelet Drug
Blocks enzyme so that platelets are unable to aggregate
Fold here

Uses
Prevention of stroke and MI
Adverse Effects
Hemorrhage

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


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

Fold here
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) ALTEPLASE (tPA)


Thrombolytic Drug
Thrombolytic Drug
Converts plasminogen to plasmin
Plasmin is an enzyme that digests the fibrin matrix of clots
Uses
Fold here

Acute myocardial infarction, pulmonary embolism, and ischemic stroke


Adverse Effects
Bleeding
Intracranial hemorrhage

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


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

Uses

Fold here
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)
Copyright © 2007 by Saunders, an imprint of Elsevier Inc.
May be used during pregnancy

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WARFARIN (COUMADIN) WARFARIN (COUMADIN)


Oral Anticoagulant
Oral Anticoagulant
Suppresses coagulation by antagonizing vitamin K
Blocks synthesis of factors VII, IX, X, and prothrombin
Effect takes a few days
Uses
Fold here

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

Fold here
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
Uses
B12 deficiency, pernicious anemia
Macrocytic normochromic anemia (megaloblastic anemia)
Fold here

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)

Fold here
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) OPRELVEKIN (INTERLEUKIN-11)


Thrombopoietic Growth Factor
Thrombopoietic Growth Factor
Stimulates production of platelets (thrombocytes)
Uses
Used in patients undergoing chemotherapy to increase platelets
Fold here

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) EPOETIN ALFA (ERYTHROPOIETIN)
Hematopoietic Growth Factor
Hematopoietic Growth Factor
Stimulates production of red blood cells
Uses
Anemia of chronic renal failure

Fold here
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) FILGRASTIM (NEUPOGEN)


Granulocyte Colony Stimulating Factor (G-CSF)
Granulocyte Colony Stimulating Factor (G-CSF)
Acts on bone marrow to increase production of neutrophils
Uses
Used in patients undergoing chemotherapy
Fold here

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) GLIPIZIDE (GLUCOTROL)
GLYBURIDE (MICRONASE) Oral Hypoglycemic Agent
GLIMEPIRIDE (AMARYL) Sulfonylurea
Stimulates insulin release from the pancreas
Oral Hypoglycemic Agents
Sulfonylureas Uses

Fold here
Type 2 diabetes
Adverse Effects
Hypoglycemia
Fetal harm

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

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METFORMIN (GLUCOPHAGE) METFORMIN (GLUCOPHAGE)


Oral Hypoglycemic Agent
Oral Hypoglycemic Agent Biguanide
Biguanide
Decreases blood sugar by decreasing production of glucose in the liver
Enhances glucose uptake and utilization in muscle
Fold here

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) ROSIGLITAZONE (AVANDIA)
PIOGLITAZONE (ACTOS) Thiazolidinedione (TZD)
“Glitazone”
Thiazolidinediones (TZDs) Insulin Sensitizer
“Glitazones”
Increases insulin sensitivity
Insulin Sensitizers

Fold here
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) MIGLITOL (GLYSET)


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

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

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

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


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

Fold here
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) PROPYLTHIOURACIL (PTU)


Antithyroid Drug
Antithyroid Drug
Inhibits thyroid hormone synthesis
Uses
Hyperthyroidism, Graves’ disease
Fold here

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
Rheumatoid arthritis, SLE, inflammatory bowel disease

Fold here
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) SILDENAFIL (VIAGRA)


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

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

Fold here
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 LIVE VIRUS VACCINES


Varicella (Varivax) Live virus vaccines are contraindicated in pregnancy
Oral Polio Vaccine (OPV) not used in the United States Give with caution in immunocompromised patients
Measles, Mumps, and Rubella Virus Vaccine (MMR)
Live Influenza Attenuated Vaccine (LIAV) Fold here

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


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

Fold here
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) METHOTREXATE (RHEUMATREX, TREXALL)


Cytotoxic Drug
Cytotoxic Drug Immunosuppressant
Immunosuppressant Disease-Modifying Antirheumatic Drug (DMARD)
Disease-Modifying Antirheumatic Drug (DMARD)
Blocks conversion of folic acid to its active form
Reduces joint destruction, retards disease progression
Fold here

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) DIPHENHYDRAMINE (BENADRYL)
First-Generation H1 Antagonist
First-Generation H1 Antagonist Antihistamine
Antihistamine
Blocks H1 receptors
Blocks some muscarinic receptors
Reduces actions of histamine

Fold here
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) LORATADINE (CLARITIN)


DESLORATADINE (CLARINEX) Second-Generation Nonsedating H1
FEXOFENADINE (ALLEGRA) Antagonist (Antihistamine)
CETIRIZINE (ZYRTEC)
Blocks H1 receptors
Reduces actions of histamine
Second-Generation Nonsedating H1 Decreases flushing, itching, secretion of mucus
Fold here

Antagonists (Antihistamines) Does not cross blood-brain barrier to cause sedation


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

Fold here
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
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Fetal harm, salicylism
Hypersensitivity in patients with allergies

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IBUPROFEN (ADVIL, MOTRIN) IBUPROFEN (ADVIL, MOTRIN)


First-Generation NSAID
First-Generation NSAID
Inhibits cyclooxygenase (COX)-1 and COX-2
Inhibits prostaglandin synthesis
Fold here Has antiinflammatory, analgesic, and antipyretic actions
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) CELECOXIB (CELEBREX)
Second-Generation NSAID
Second-Generation NSAID COX-2 Inhibitor
COX-2 Inhibitor
Selective inhibition of COX-2, decreases prostaglandin synthesis (pain
and inflammation reduced)
Spares COX-1 inhibition

Fold here
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) ACETAMINOPHEN (TYLENOL)


Analgesic
Analgesic Antipyretic
Antipyretic
Decreases prostaglandin synthesis in the CNS
Devoid of antiinflammatory properties
Fold here

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) FLUTICASONE PROPIONATE (FLOVENT)
Inhaled Corticosteroid (ICS)
Inhaled Corticosteroid (ICS)
Suppresses inflammation
Decreases leukotrienes, histamine, and prostaglandins
Decreases eosinophils and leukocytes
Reduces edema of airway and mucous production

Fold here
Reduces bronchial hyperactivity
Increases number and responsiveness of beta2 receptors
Uses
Asthma
Adverse Effects
Oropharyngeal candidiasis—rinse mouth after use
Minimal adrenal suppression and bone loss
Slows growth but does not reduce adult height
Copyright © 2007 by Saunders, an imprint of Elsevier Inc. Slight increased risk of cataracts and glaucoma

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SALMETEROL (SEREVENT) SALMETEROL (SEREVENT)


Long-Acting Inhaled Beta2-Adrenergic Agonist
Long-Acting Inhaled Beta2-Adrenergic Agonist
Activates beta2 receptors in the lung
Promotes bronchodilation
Suppresses histamine release in the lung
Increases ciliary motility
Fold here

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) MONTELUKAST (SINGULAIR)
Leukotriene Modifier
Leukotriene Modifier
Blocks leukotriene receptors
Decreases inflammation, bronchoconstriction, and edema
Decreases mucous secretion
Decreases eosinophils and other inflammatory cells

Fold here
Reduces dosage of inhaled corticosteroid (ICS)
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 THEOPHYLLINE
Methylxanthine
Methylxanthine Bronchodilator
Bronchodilator
Produces bronchodilation by relaxing bronchi
Uses
Fold here

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

Fold here
Uses
Asthma
Adverse Effects
Hyperglycemia, tachycardia, tremor

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

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RANITIDINE (ZANTAC) RANITIDINE (ZANTAC)


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

Histamine2-Receptor Antagonists Uses


Fold here

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) OMEPRAZOLE (PRILOSEC)
LANSOPRAZOLE (PREVACID) Proton Pump Inhibitor (PPI)
RABEPRAZOLE (ACIPHEX)
PANTOPRAZOLE (PROTONIX) Inhibits the enzyme that generates acid production
ESOMEPRAZOLE (NEXIUM) Uses
Duodenal and gastric ulcers, GERD, dyspepsia

Fold here
Proton Pump Inhibitors (PPIs) 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) SUCRALFATE (CARAFATE)


Antiulcer drug
Antiulcer drug
Creates a protective barrier against acid and pepsin
Sticky gel adheres to ulcer crater
Uses
Fold here

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

Fold here
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) SULFASALAZINE (AZULFIDINE)


Aminosalicylate
Aminosalicylate
Reduces inflammation
Uses
Inflammatory bowel disease
Fold here

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

Fold here
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) PROCHLORPERAZINE (COMPAZINE)


PROMETHAZINE (PHENERGAN) Antiemetic Drug
Dopamine Antagonist
Antiemetic Drugs
Suppresses emesis by blocking dopamine2 receptors in the CTZ
Dopamine Antagonists
Uses
Fold here

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

Fold here
Nausea
Adverse Effects
Sedation, blurry vision, urinary retention, dry mouth

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PENICILLIN G (BENZYLPENICILLIN) PENICILLIN G (BENZYLPENICILLIN)


Narrow-Spectrum Penicillin
Narrow-Spectrum Penicillin
Weakens the bacterial cell wall
Uses
Treats Streptococcus, Neisseria, anaerobes, and others
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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) NAFCILLIN (UNIPEN)
Penicillinase-Resistant Penicillin
Penicillinase-Resistant Penicillin (Antistaphylococcal Penicillin)
(Antistaphylococcal Penicillin)
Weakens the cell wall
Uses

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Treats infections caused by Staphylococcus aureus
Adverse Effects
Allergic reaction, GI effects
Thrombophlebitis, hypokalemia

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AMOXICILLIN (AMOXIL) AMOXICILLIN (AMOXIL)


Broad-Spectrum Penicillin (Aminopenicillin)
Broad-Spectrum Penicillin (Aminopenicillin)
Weakens the bacterial cell wall
Uses
Treats infections caused by Haemophilus influenzae, Escherichia coli,
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Proteus mirabilis, enterococci


Neisseria gonorrhoeae
Adverse Effects
Diarrhea

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


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

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Gram-positive infections
Surgical prophylaxis
Adverse Effects
Allergic reaction
Bleeding tendencies
Thrombophlebitis
Antibiotic-associated pseudomembranous colitis (AAPMC)

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CEFUROXIME (CEFTIN) CEFUROXIME (CEFTIN)


Second-Generation Cephalosporin
Second-Generation Cephalosporin Beta-Lactam Antibiotic
Beta-Lactam Antibiotic
Weakens the bacterial cell wall
Uses
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Upper respiratory tract infections


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

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

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Active against gram-negative organisms
Adverse Effects
Allergic reaction
Bleeding tendencies
Thrombophlebitis
Antibiotic-associated pseudomembranous colitis (AAPMC)

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VANCOMYCIN (VANCOCIN) VANCOMYCIN (VANCOCIN)


Antibiotic
Antibiotic
Inhibits bacterial cell wall synthesis
Uses
Active against gram-positive bacteria
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Serious infections, such as methicillin-resistant Staphylococcus


aureus (MRSA)
Antibiotic-associated pseudomembranous colitis (AAPMC)
Used for patients allergic to penicillin
Adverse Effects
Ototoxicity
Rapid infusion can lead to “red man syndrome” (flushing, tachycardia,
and hypotension)
Infuse over 60 minutes or more
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TETRACYCLINE TETRACYCLINE
DOXYCYCLINE Broad-Spectrum Antibiotic
MINOCYCLINE
Suppresses bacterial growth by inhibiting protein synthesis
Broad-Spectrum Antibiotics Uses
Rocky Mountain spotted fever, typhus

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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

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ERYTHROMYCIN ERYTHROMYCIN
CLARITHROMYCIN (BIAXIN) Macrolide Antibiotic
AZITHROMYCIN (ZITHROMAX) Broad-Spectrum Antibiotic
DIRITHROMYCIN (DYNABAC)
TELITHROMYCIN (KETEK) Inhibits bacterial cell wall synthesis
Uses
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Macrolide Antibiotics Active against most gram-positive and some gram-negative organisms
Broad-Spectrum Antibiotics 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

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CLINDAMYCIN (CLEOCIN) CLINDAMYCIN (CLEOCIN)
Antibiotic
Antibiotic
Inhibits bacterial protein synthesis
Uses
Active against most anaerobic bacteria outside the CNS

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Bacteroides fragilis, Fusobacterium, Clostridium perfringens
Adverse Effects
Antibiotic-associated pseudomembranous colitis (AAPMC)
Diarrhea

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GENTAMICIN (GARAMYCIN) GENTAMICIN (GARAMYCIN)


AMIKACIN (AMIKIN) Aminoglycoside Antibiotic
TOBRAMYCIN (NEBCIN) Narrow-Spectrum Antibiotic
Disrupts bacterial protein synthesis
Aminoglycoside Antibiotics
Narrow-Spectrum Antibiotics Uses
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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 TRIMETHOPRIM/SULFAMETHOXAZOLE
(TMP-SMZ-BACTRIM) (TMP-SMZ-BACTRIM)
Antibiotic
Antibiotic
Combination antibiotic that inhibits bacterial synthesis of folic acid
Uses

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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

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CIPROFLOXACIN (CIPRO) CIPROFLOXACIN (CIPRO)


MOXIFLOXACIN (AVELOX) Fluoroquinolone Antibiotic
GATIFLOXACIN (TEQUIN)
LEVOFLOXACIN (LEVAQUIN) Inhibits bacterial DNA
Uses
Fluoroquinolone Antibiotics Infections of the urinary, respiratory, and GI tracts; bones; joints; skin;
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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) METRONIDAZOLE (FLAGYL)
Antibacterial Drug
Antibacterial Drug
Causes cell death by damaging bacterial DNA
Uses
Protozoal infection

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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
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KETOCONAZOLE (NIZORAL) KETOCONAZOLE (NIZORAL)


FLUCONAZOLE (DIFLUCAN) Antifungal Agent
ITRACONAZOLE (SPORANOX)
MICONAZOLE (MONISTAT) Causes bacterial cell wall to leak
CLOTRIMAZOLE Uses
Systemic and superficial mycoses (fungi)
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Antifungal Agents
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 GRISEOFULVIN
Antifungal Agent
Antifungal Agent
Inhibits fungal mitosis
Uses
Superficial mycoses (fungi)

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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

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ACYCLOVIR (ZOVIRAX) ACYCLOVIR (ZOVIRAX)


VALACYCLOVIR (VALTREX) Antiviral Agent
FAMCICLOVIR (FAMVIR)
Suppresses synthesis of viral DNA
Antiviral Agents Uses
Herpesvirus, varicella-zoster virus, cytomegalovirus (CMV)
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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

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INTERFERON ALPHA INTERFERON ALPHA
Antiviral Agent
Antiviral Agent
Decreases viral replication
Uses
Hepatitis B and C

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Adverse Effects
Flulike syndrome
Depression
Fatigue, hair loss, thyroid damage, heart damage
Bone marrow suppression

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RIBAVIRIN (REBETOL) RIBAVIRIN (REBETOL)


Antiviral Agent
Antiviral Agent
Uses
Fold here Used with interferon for treatment of hepatitis C
Adverse Effects
Hemolytic anemia
Fetal harm (Category X)
Use second reliable form of birth control during treatment and 6 months
after treatment

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


NUCLEOSIDE REVERSE TRANSCRIPTASE NUCLEOSIDE REVERSE TRANSCRIPTASE
INHIBITORS (NRTIs) INHIBITORS (NRTIs)
Antiretroviral Drugs
Zidovudine (Retrovir)
Suppress the synthesis of viral DNA by blocking transcriptase
Lamivudine (Epivir)
Zalcitabine (Hivid) Uses

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Antiretroviral Drugs HIV infection
Adverse Effects
Anemia, neutropenia, lactic acidosis

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NON-NUCLEOSIDE REVERSE TRANSCRIPTASE NON-NUCLEOSIDE REVERSE TRANSCRIPTASE


INHIBITORS (NNRTIs) INHIBITORS (NNRTIs)
Delavirdine (Rescriptor) Antiretroviral Drugs
Efavirenz (Sustiva)
Nevirapine (Viramune) Inhibit reverse transcriptase by binding to it
Uses
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Antiretroviral Drugs HIV infection


Adverse Effects
Rash, Stevens-Johnson syndrome, erythema multiforme
Hepatotoxicity

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PROTEASE INHIBITORS PROTEASE INHIBITORS
Nelfinavir (Viracept) Antiretroviral Drugs
Ritonavir (Norvir)
Saquinavir (Invirase) Inhibit the enzyme protease, needed for HIV to mature
Uses
Antiretroviral Drugs HIV

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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

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