(Pharmacology) Drug Cards

Common Drug Endings-cont’d Common Drug Endings
Drug Endings Drug Classification Drug Example Drug Endings Drug Classification Drug Example
-tidine Histamine2 blocker-acid reducer Cimetidine -zosin Alpha-adrenergic blocker used for HTN and BPH Prazosin
-prazole Protein pump inhibitor-acid reducer Omeprazole -olol, -lol Beta-adrenergic blocker (BB) Metoprolol
-cillin Penicillin antibiotic Amoxicillin -zepam, -zolam Benzodiazepine (BZD) Diazepam,
cef-, ceph- Cephalosporin antibiotic Cefazolin alprazolam
-cycline Tetracycline antibiotic Tetracycline -pril Angiotensin-converting enzyme (ACE) inhibitor Lisinopril
-floxacin Fluoroquinolone antibiotic Levofloxacin -artan Angiotensin-receptor blocker (ARB) Candesartan
-thromycin Macrolide antibiotic Azithromycin -dipine Calcium channel blocker (CCB) Amlodipine
-micin, mycin Aminoglycoside antibiotic Gentamicin -statin Lipid-lowering drug Atorvastatin
Fold here
-azole Antifungal Itraconazole -ase, -plase Thrombolytic used to dissolve clots Alteplase
-triptan Serotonin-receptor agonists used for migraines Sumatriptan -parin Anticoagulant Enoxaparin
-denafil, -dalafil PED5 inhibitors for erectile dysfunction Sildenafil -sone Corticosteroid Prednisone
-curium, Neuromuscular blockers used for muscle Pancuronium -dronate Bisphosphonate for osteoporosis Alendronate
-curonium relaxation during surgery -terol Bronchodilator used for asthma and COPD Albuterol
HTN, Hypertension; BPH, benign prostatic hypertrophy; COPD, chronic obstructive pulmonary Continued
disease; PED5, Phosphodiesterase type 5.
Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

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DRUGS THAT SHOULD BE AVOIDED DURING DRUGS THAT SHOULD BE AVOIDED DURING
Ch 9 Drug Therapy During Pregnancy and Breast-Feeding

PREGNANCY BECAUSE OF PREGNANCY BECAUSE OF
PROVEN OR STRONGLY SUSPECTED PROVEN OR STRONGLY SUSPECTED
TERATOGENICITY TERATOGENICITY
Anticancer/Immunosuppressants drugs (methotrexate) The risks for most drugs used in pregnancy have not been determined.
Antiseizure drugs (carbamazepine, valproic acid, phenytoin, and others)
Androgens (danazol, finasteride, dutasteride) (The benefits of treatment must balance the risks.)
ACE inhibitors (lisinopril and others) Category A: Remote risk of fetal harm
Angiotensin-receptor blockers (losartan and others) Category B: Slightly more risk than A
Fold here
Antithyroid drugs (propylthiouracil, methimazole) Category C: Greater risk than B

Fluoroquinolone antibiotics (ciprofloxacin, levofloxacin) Category D: Proven risk of fetal harm
HMG-CoA reductase inhibitors [ie, statins] (atorvastatin and others) Category X: Proven risk of fetal harm
Isotretinoin (Accutane) used for acne
Lithium used for bipolar disorder
Nonsteroidal anti-inflammatory drugs (ibuprofen and others)
Megadoses of vitamin A
Tetracycline antibiotics (minocycline, doxycycline)
Warfarin (Coumadin)

Functions of Peripheral Cholinergic Receptor Subtypes Functions of Peripheral Adrenergic Receptor Subtypes
CH 13 Physiology of he Peripheral Nervous System

Receptor Receptor
Subtype Location Response to Receptor Activation Subtype Location Response to Receptor Activation
Nicotinicn All autonomic nervous system Stimulation of parasympathetic and Alpha1 Eye Mydriasis: “Wide eyed with fear”
ganglia and the adrenal medulla sympathetic postganglionic nerves and Arterioles and veins (skin, viscera, Constriction: (BP increases), blood is
release of epinephrine from the adrenal mucous membranes) shunted away from the skin and viscera into
medulla skeletal muscle; “cold with fear”
Nicotinicm Neuromuscular junction Contraction of skeletal muscle Sex organs, male Ejaculation
Muscarinic All parasympathetic target organs: Bladder neck and prostatic capsule Contraction
Eye Miosis (pupils constrict) Alpha2 Presynaptic nerve terminals Inhibition of transmitter release (NE):
Fold here
Heart Decreased rate Decreased sympathetic nervous system
Lung Constriction of bronchi (SNS) outflow to the blood vessels and
Promotion of secretions heart reduces BP and pain
Bladder Voiding of the urinary bladder Beta1 Heart Increase in rate and force of contraction and
Gastrointestinal (GI) tract Salivation in AV conduction velocity
Increases gastric secretions, intestinal tone, Kidney Release of renin to raise BP
and motility Beta2 Arterioles (heart, lung, and skeletal Dilation increases blood flow to organs
Defecation muscle)
Sweat glands Generalized sweating Bronchi Dilation improves oxygenation
Sex organs Erection Uterus Relaxation prevents labor
Blood vessels Vasodilation (BP decreases) Liver Glycogenolysis increases blood glucose
Skeletal muscle Enhanced contraction, glycogenolysis
Dopamine Kidney Dilation of kidney vasculature
NE, Norepinephrine; AV, atrioventricular.
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MUSCARINIC AGONISTS MUSCARINIC AGONISTS
Ch 14 Muscarinic Agonists and Antagonists

Prototype: Bethanechol (Urecholine) Prototype: Bethanechol (Urecholine)
Mechanism of Action
Activates muscarinic receptors
Other Muscarinic Agonists
Causes contraction of the detrusor muscle of the bladder and Cevimeline (Evoxac) for xerostomia (dry mouth)
relaxation of the trigone and sphincter; the result is bladder emptying and inflammation of the cornea and conjunctiva
Pilocarpine for topical therapy of glaucoma
Uses Muscarine is found in poisonous mushrooms
Postoperative and postpartum urinary retention
Fold here
Adverse Effects
Hypotension due to vasodilation and bradycardia
GI effects (excessive salivation, increased gastric acid, cramps, and diarrhea)
Bladder rupture in patients with urinary obstruction
Exacerbation of asthma due to bronchoconstriction
Dysrhythmias in hyperthyroid patients due to reflex tachycardia

MUSCARINIC POISONING MUSCARINIC POISONING

Manifestation of Muscarinic Poisoning
Stimulation of muscarinic receptors causes profuse salivation,
lacrimation (tearing), visual disturbances,
bronchospasm, diarrhea, bradycardia,
hypotension, and cardiovascular collapse
Sources of Muscarinic Poisoning

Ingestion of Inocybe and Clitocybe mushrooms
Fold here
Overdose with direct-acting muscarinic agonists (bethanechol, pilocarpine)
Overdose with cholinesterase inhibitors (neostigmine [Prostigmin])
Treatment
Administration of atropine (a muscarinic blocking agent)
Supportive care

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MUSCARINIC ANTAGONISTS MUSCARINIC ANTAGONISTS

(ANTICHOLINERGIC DRUGS) (ANTICHOLINERGIC DRUGS)
Prototype: Atropine Prototype: Atropine
Mechanism of Action
Blocks muscarinic receptors Other Muscarinic Antagonists
Prevents receptor activation by endogenous acetylcholine
Increases heart rate (tachycardia) Drugs for an overactive bladder (eg, oxybutynin [Ditropan])
Decreases salivary, bronchial, sweat, and acid-secreting cell secretions Scopolamine for motion sickness
Relaxes bronchial smooth muscles (bronchodilation) Ipratropium bromide (Atrovent) for COPD, rhinitis, and asthma
Decreases bladder tone and GI motility (urinary retention) Antisecretory anticholinergics (glycopyrrolate [Robinul])
Dilates pupils (mydriasis)
Fold here
Cycloplegia (relaxation of the ciliary muscle) Dicyclomine (Bentyl) for irritable bowel syndrome
Mild central nervous system (CNS) excitation, hallucinations, and delirium Centrally acting anticholinergics for Parkinson’s disease:
(trihexyphenidyl [Artane] and benztropine [Cogentin])
Uses
Preanesthesia to prevent bradycardia
Dilation of pupil for ocular examination or surgery
Treatment of bradycardia
Intestinal hypertonicity and hypermotility for dysentery
Antidote for muscarinic agonist poisoning
Adverse Effects
Blurry vision, photophobia, increased intraocular pressure
Urinary retention, dry mouth, constipation
Anhidrosis and tachycardia (BUDCAT)
ANTICHOLINERGIC SIDE EFFECTS ANTICHOLINERGIC SIDE EFFECTS

B- blurry vision, photophobia, and increased intraocular pressure B
U- urinary retention
D- dry mouth (xerostomia), decreased secretions
U
C- constipation D
A- anhidrosis (absence of sweat) C
T- tachycardia A
Other Drugs with Anticholinergic Side Effects T
First-generation antihistamines (diphenhydramine [Benadryl])
Fold here
Antiemetics (prochlorperazine [Compazine], promethazine [Phenergan])
First- and second-generation antipsychotic agents
Tricyclic antidepressants (imipramine [Tofranil])

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ANTICHOLINERGIC DRUGS FOR OVERACTIVE ANTICHOLINERGIC DRUGS FOR OVERACTIVE

BLADDER (OAB) BLADDER (OAB)
Prototype: Oxybutynin Prototype: Oxybutynin
(Ditropan, Ditropan XL, Oxytrol) (Ditropan, Ditropan XL, Oxytrol)
Mechanism of Action
Blocks muscarinic (M3) receptors in the bladder
Other Anticholinergic Drugs for OAB
Inhibits bladder contractions and the urge to void Darifenacin (Enablex)
Solifenacin (Vesicare)
Uses Tolterodine (Detrol, Detrol LA)
Fold here
Overactive bladder (urge incontinence) Trospium (Sanctura, Sanctura XR)
Adverse Effects
Blurry vision, photophobia, increased intraocular pressure
Urinary retention, dry mouth, constipation
Anhidrosis and tachycardia (BUDCAT)
CNS effects

CHOLINESTERASE INHIBITORS CHOLINESTERASE INHIBITORS
Ch 15 Cholinesterase Inhibitors and Their Use in Myasthenia Gravis

Prototype: Neostigmine (Prostigmin) Prototype: Neostigmine (Prostigmin)
Mechanism of Action
Prevents degradation of acetylcholine (ACh)
Other Reversible Cholinesterase Inhibitors
ACh accumulates at neuromuscular junction Ambenonium (Mytelase)
Enhances effect of ACh to stimulate skeletal muscle contraction Pyridostigmine (Mestinon)
Muscarinic receptor activation Edrophonium (Tensilon)
Physostigmine (Antilirium) for anticholinergic poisoning
Uses Echothiophate for treatment of glaucoma
Fold here
Myasthenia gravis
Reversal of neuromuscular blockade in postoperative patients
Cholinesterase Inhibitors Used
Glaucoma, Alzheimer’s disease, and poisoning by muscarinic antagonists to Treat Alzheimer’s Disease
Donepezil (Aricept)
Adverse Effects Galantamine (Razadyne)
Excessive glandular secretions, increased GI motility Rivastigmine (Exelon)
Urinary urgency, bradycardia, sweating, and miosis Tacrine (Cognex)
Toxic doses reduce force of muscle contraction
Cholinergic crisis—treat with atropine

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NEUROMUSCULAR BLOCKERS
Ch 16 Drugs That Block Nicotinic Cholinergic Transmission

Prototype: Succinylcholine (Anectine, Quelicin) NEUROMUSCULAR BLOCKERS
(Depolarizing neuromuscular blocker) Prototype: Succinylcholine (Anectine, Quelicin)
(Depolarizing neuromuscular blocker)
Mechanism of Action
Causes paralysis of muscle by preventing repolarization (fasciculations) Nondepolarizing Neuromuscular Blockers
Atracurium (Tracrium)
Uses Cisatracurium (Nimbex)
Muscle relaxation during endotracheal intubation Pancuronium
Rocuronium (Zemuron)
Fold here
Short operative procedures

Facilitation of mechanical ventilation Vecuronium (Norcuron)
Adjunct to electroconvulsive therapy
Diagnosis of myasthenia gravis
Adverse Effects
Prolonged paralysis in genetically determined individuals
Hypotension
Malignant hyperthermia—treat with dantrolene
Hyperkalemia with cardiac arrest
Muscle pain
Antibiotics can intensify effect
ADRENERGIC AGONISTS ADRENERGIC AGONISTS
Ch 17 Adrenergic Agonists
Prototype: Epinephrine Prototype: Epinephrine
Mechanism of Action
Activates all four adrenergic receptors (alpha1, alpha2, beta1, and beta2)
Other Adrenergic Agonists
Pupil dilation, arterial and venous vasoconstriction (Catecholamines and noncatecholamines)
Increases heart rate and force of contraction
Bronchial dilation, glycogenolysis, enhanced muscle contraction Norepinephrine (Levophed)
Isoproterenol (Isuprel)
Uses Dopamine
Fold here
Cardiac arrest, heart failure, anaphylactic shock Dobutamine
AV heart block and asthma Phenylephrine
Delays absorption of local anesthetic and controls superficial bleeding Terbutaline
Dilates pupil (mydriasis) for eye procedures Ephedrine
Adverse Effects
Hypertensive crisis, dysrhythmias, angina pectoris
Necrosis after extravasation
Hyperglycemia in diabetic patients

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ADRENERGIC AGONISTS ADRENERGIC AGONISTS
Ch 17 Adrenergic Agonists
Prototype: Phenylephrine Prototype: Phenylephrine
(Noncatecholamine) (Noncatecholamine)
Mechanism of Action Other Sympathomimetics Used for Nasal Congestion

Activates alpha1 receptors Oxymetazoline (Afrin)
Constricts blood vessels of the skin, viscera, and mucous membranes Pseudoephedrine (Sudafed)
Uses
Fold here
Treatment of nasal congestion

Delay of anesthetic absorption
Dilation of the pupil for ocular exam
Adverse Effects
Hypertension
Necrosis

ALPHA-ADRENERGIC ANTAGONISTS ALPHA-ADRENERGIC ANTAGONISTS
Ch 18 Adrenergic Antagonists
Prototype: Prazosin (Minipress) Prototype: Prazosin (Minipress)
Mechanism of Action
Blocks alpha1 receptors
Other Alpha Blockers
Dilates arteries and veins Terazosin (Hytrin)
Relaxes smooth muscle in the bladder neck and prostatic capsule Doxazosin (Cardura)
Tamsulosin (Flomax) for BPH only
Uses Alfuzosin (Uroxatral) for BPH only
Essential hypertension Phentolamine for tissue necrosis
Fold here
Reversal of toxicity from alpha1 agonists
Benign prostatic hyperplasia
Pheochromocytoma
Raynaud’s disease
Adverse Effects
Orthostatic hypotension, reflex tachycardia
Nasal congestion
Inhibition of ejaculation
Use with sildenafil (Viagra) can lead to hypotension
Sodium retention and increased blood volume
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BETA-ADRENERGIC ANTAGONISTS BETA-ADRENERGIC ANTAGONISTS
First-Generation Nonselective Beta Blockers First-Generation Nonselective Beta Blockers
Prototype: Propranolol (Inderal, InnoPran) Prototype: Propranolol (Inderal, InnoPran)
Mechanism of Action
Blocks beta1 and beta2 receptors Other First-Generation Nonselective Beta Blockers
Reduces heart rate, decreases force of ventricular contraction Nadolol (Corgard)
Decreases conduction through AV node, decreases cardiac output Sotalol (Betapace) for dysrhythmias
Suppresses secretion of renin Carvedilol (Coreg) blocks beta1, beta2, and alpha1 receptors
Bronchoconstriction through beta2 blockade in the lung
Fold here
Labetalol (Trandate) blocks beta1, beta2, and alpha1 receptors

Reduces glycogenolysis through beta2 blockade in muscle and liver
Uses
Hypertension, angina pectoris, cardiac dysrhythmias
Myocardial infarction, hyperthyroidism
Migraine headache prophylaxis, “stage fright”
Adverse Effects
Bradycardia, AV heart block, heart failure
Rebound cardiac excitation (tachycardia) after abrupt withdrawal
Bronchoconstriction in asthmatics
Inhibition of glycogenolysis, CNS effects mask tachycardia
associated with hypoglycemia indicated in diabetics
Avoid in patients with asthma, diabetes, depression, or severe allergies Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
Second-Generation Cardioselective Beta Blockers Second-Generation Cardioselective Beta Blockers
Prototype: Metoprolol (Lopressor, Toprol XL) Prototype: Metoprolol (Lopressor, Toprol XL)
Mechanism of Action
Blocks cardiac beta1 receptors
Other Cardioselective Beta Blockers
Reduces heart rate, decreases force of ventricular contraction Acebutolol (Sectral)
Decreases conduction through AV node, decreases cardiac output Atenolol (Tenormin)
Suppresses renin Betaxolol (Kerlone)
Fold here
Minimal blockade of beta2 receptors (less bronchoconstriction) Bisoprolol (Zebeta)
Not likely to inhibit glycogenolysis Esmolol (Brevibloc) for dysrhythmias
Preferred for patients with asthma or diabetes
Uses
Hypertension, angina pectoris, heart failure
Myocardial infarction
Adverse Effects
Bradycardia, reduction of cardiac output, AV heart block
Rebound cardiac excitation (tachycardia) after abrupt withdrawal
Masks tachycardia associated with hypoglycemia in diabetics Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
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Third-Generation Vasodilating Third-Generation Vasodilating
Alpha and Beta Blockers Alpha and Beta Blockers
Prototype: Labetalol (Normodyne, Trandate) Prototype: Labetalol (Normodyne, Trandate)
Mechanism of Action
Blocks alpha1 receptors on veins, causing vasodilation
Other Alpha and Beta Blockers
Blocks beta1 receptors in the heart and beta2 receptors in the lung Carvedilol (Coreg) for heart failure
(blocks beta1, beta2, and alpha1 receptors)
Fold here
Uses Nebivolol (Bystolic) blocks beta receptors

Hypertension, hypertensive crisis (promotes release of nitric acid, a vasodilator)
Adverse Effects
Dizziness, orthostatic hypotension, ventricular dysrhythmias
Nasal congestion, sexual dysfunction,
bronchospasm

CENTRALLY ACTING ALPHA2 AGONISTS CENTRALLY ACTING ALPHA2 AGONISTS
Ch 19 Indirect-Acting Antiadrenergic Agents

Prototype: Clonidine (Catapres) Prototype: Clonidine (Catapres)
Mechanism of Action
Activates alpha2 receptors in the CNS
Other Alpha2 Agonists
Reduces sympathetic outflow to the heart and blood vessels Guanabenz (Wytensin)
Reduces stimulation of adrenergic receptors in the periphery Guanfacine (Tenex)
Net effect of cardiac suppression and vasodilation is decreased blood pressure Methyldopa*
*Adverse effects of methyldopa are hemolytic anemia and hepatotoxicity
Uses
Fold here
Hypertension A positive Coombs’ test can occur with methyldopa
Epidural infusion to relieve severe cancer pain
Adverse Effects
Drowsiness and sedation
Xerostomia (dry mouth)
Hypotension
Bradycardia, decrease in cardiac output
Rebound hypertension in response to abrupt withdrawal
Fetal harm

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DOPAMINERGICS FOR PARKINSON’S DISEASE DOPAMINERGICS FOR PARKINSON’S DISEASE
Ch 21 Drugs for Parkinson’s Disease

Prototype: Levodopa/Carbidopa (Sinemet) Prototype: Levodopa/Carbidopa (Sinemet)
Mechanism of Action
Levodopa increases synthesis of dopamine in the striatum
Other Drugs That Increase Dopamine
Carbidopa enhances effect of levodopa Pramipexole (Mirapex)
Ropinirole (Requip)
Uses Entacapone (Comtan)
Reduces symptoms of Parkinson’s disease Selegiline (Eldepryl)
Amantadine (Symmetrel)
Fold here
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

CHOLINESTRASE INHIBITORS FOR CHOLINESTRASE INHIBITORS FOR
Ch 22 Alzheimer’s Disease
ALZHEIMER’S DISEASE ALZHEIMER’S DISEASE
Prototype: Donepezil (Aricept) Prototype: Donepezil (Aricept)
Mechanism of Action
Prevents the breakdown of acetylcholine (ACh)
Other Cholinesterase Inhibitors
Increases ACh at cholinergic synapses Tacrine (Cognex) rarely used due to hepatotoxicity
May slow progression of Alzheimer’s disease Rivastigmine (Exelon)
Minimal improvement of memory and cognitive function Galantamine (Razadyne)
Other Drugs for Alzheimer’s Disease
Fold here
Uses
Alzheimer’s disease Memantine (Namenda)
N-methyl-D-aspartate (NMDA)–receptor antagonists for moderate
Adverse Effects to severe disease
Cholinergic effects
Nausea, vomiting, dyspepsia, diarrhea
Bradycardia
Bronchoconstriction

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ANTIEPILEPTIC DRUGS (AEDs) ANTIEPILEPTIC DRUGS (AEDs)
Ch 24 Drugs for Epilepsy

Prototype: Phenytoin (Dilantin) Prototype: Phenytoin (Dilantin)
Mechanism of Action
Inhibits entry of sodium into neurons Other AEDs
Suppresses action potential of neurons Carbamazepine (Tegretol)
Valproic acid (Depakene, Depakote, Depacon)
Uses Ethosuximide (Zarontin)
Epilepsy
Phenobarbital
Cardiac dysrhythmias
Fosphenytoin (Cerebyx), a prodrug form of phenytoin
Fold here
Adverse Effects
Nystagmus, sedation, ataxia, diplopia, cognitive impairment
Gingival hyperplasia, rash, hirsutism, liver damage
Fetal harm, bleeding tendencies in newborns
Narrow therapeutic range (10 to 20 mcg/mL)
Inject slowly (do not exceed 50 mg/minute)
Dysrhythmias and hypotension if injected too fast
Use normal saline to prevent precipitation
Induces the metabolism of other drugs such as:
oral contraceptives, warfarin, and glucocorticoids (drug effect is decreased)
Withdraw over 6 to 8 weeks to prevent seizures
All AEDs may increase suicidal thoughts and behaviors

ANTIEPILEPTIC DRUGS (AEDs) ANTIEPILEPTIC DRUGS (AEDs)
Ch 24 Drugs for Epilepsy

Prototype: Valproic Acid (Depakote) Prototype: Valproic Acid (Depakote)
Mechanism of Action
Blocks sodium channels to suppress neurons
Newer Antiepileptic Drugs
Suppresses calcium influx Oxcarbazepine (Trileptal)
Increases inhibitory influence of gamma-aminobutyric acid (GABA) Lamotrigine (Lamictal)
Gabapentin (Neurontin)
Uses Pregabalin (Lyrica)
Epilepsy, bipolar disorder, migraine headaches Levetiracetam (Keppra)
Fold here
Topiramate (Topamax)
Adverse Effects Tiagabine (Gabitril)
Zonisamide (Zonegran)
Nausea, vomiting, indigestion
Felbamate (Felbatol)
Hepatotoxicity, pancreatitis, fetal harm
Vigabatrin (Sabril)
Weight gain, rash, hair loss, tremor
Blood dyscrasias

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MUSCLE RELAXANTS MUSCLE RELAXANTS
Ch 25 Drugs for Muscle Spasm and Spasticity

Prototype: Metaxalone (Skelaxin) Prototype: Metaxalone (Skelaxin)
Mechanism of Action
Unclear; sedative properties may cause relaxation
Other Centrally Acting Muscle Relaxants
Baclofen (Lioresal)
Uses Diazepam (Valium)
Relief of spasm resulting from muscle injury Dantrolene
Carisoprodol (Soma)
Adverse Effects Cyclobenzaprine (Flexeril, Fexmid)
Fold here
CNS depression Cyclobenzaprine ER (Amrix)

Hepatotoxicity Chlorzoxazone (Paraflex, Parafon Forte, Remular-S)
Physical dependence Methocarbamol (Robaxin)
Orphenadrine (Norflex)
Tizanidine (Zanaflex)

LOCAL ANESTHETICS LOCAL ANESTHETICS
Ch 26 Local Anesthetics
Prototype: Lidocaine Prototype: Lidocaine
Mechanism of Action
Stops axonal conduction by blocking sodium channels in axonal membrane
Other Local Anesthetics
Stops nerve conduction Procaine (Novocain)
Bupivacaine (Marcaine)
Uses
Surgical anesthesia
Fold here
Adverse Effects
Central nervous system excitation followed by depression
Convulsions, respiratory depression
Bradycardia, heart block, reduced contractile force
Cardiac arrest, hypotension, allergic reactions

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GENERAL ANESTHESTICS GENERAL ANESTHETICS
Ch 27 General Anesthetics
Inhaled Anesthetics
Mechanism of Action
Halothane (Fluothane)
Enhance transmission at inhibitory synapses (GABA) Isoflurane (Forane)
Depress transmission at excitatory synapses (NMDA) Enflurane (Ethrane)
Desflurane (Suprane)
Uses
Sevoflurane (Ultane)
Surgery Nitrous oxide
Adverse Effects Intravenous Anesthetics
Fold here
Respiratory and cardiac depression Thiopental sodium (Pentothal)

Sensitization of the heart to catecholamines, leading to dysrhythmias Methohexital sodium (Brevital)
Malignant hyperthermia—treat with dantrolene Diazepam (Valium)
Aspiration of gastric contents Midazolam (Versed)
Toxicity to operating room personnel Propofol (Diprivan)
Hepatotoxicity Etomidate (Amidate)
Ketamine (Ketalar)
Droperidol plus fentanyl (Innovar)

OPIOID ANALGESICS OPIOID ANALGESICS
Ch 28 Opioid (Narcotic) Analgesics and Antagonists

Prototype: Morphine Prototype: Morphine
Mechanism of Action
Activates mu receptors
Other Strong Opioid Agonists
Produces analgesia, euphoria, sedation Fentanyl (Sublimaze, Duragesic, Fentora, Actiq, Ionsys)
Alfentanil (Alfenta) sufentanil (Sufenta)
Uses Remifentanil (Ultiva)
Relief of pain Meperidine (Demerol)
Methadone (Diskets, Dolophine, Methadose)
Fold here
Adverse Effects Heroin
Hydromorphone (Dilaudid)
Respiratory depression, constipation
Oxymorphone (Opana)
Orthostatic hypotension, urinary retention, cough suppression
Levorphanol (Levo-Dromoran)
Biliary colic, emesis, elevation of intracranial pressure
Euphoria, dysphoria, sedation, miosis, neurotoxicity Moderate to Strong Opioid Agonists
Tolerance and physical dependence
Prolonged use affects hormone and immune functions Codeine
Reversed with naloxone (Narcan) Oxycodone (OxyContin, Percodan, Percocet)
Hydrocodone (Vicodin, Lortab)
Propoxyphene (Darvon)

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AGONIST-ANTAGONIST OPIOIDS AGONIST-ANTAGONIST OPIOIDS

Prototype: Pentazocine (Talwin) Prototype: Pentazocine (Talwin)
Mechanism of Action
Acts as an agonist at kappa receptors and antagonist at mu receptors
Other Partial Agonists
Produces analgesia and sedation Nalbuphine (Nubain)
Mild respiratory depression, increased cardiac work Butorphanol (Stadol)
Buprenorphine (Buprenex, Subutex, Suboxone)
Uses
Relief of mild to moderate pain
Fold here
Adverse Effects
Physical dependence
Unpleasant reactions (anxiety, strange thoughts, nightmares, hallucinations)
If administered to a patient physically dependent on a pure opioid agonist,
withdrawal syndrome can occur

OPIOID ANTAGONISTS OPIOID ANTAGONISTS

Prototype: Naloxone (Narcan) Prototype: Naloxone (Narcan)
Mechanism of Action
Reverses the effects of opioids
Other Opioid Antagonists
Methylnaltrexone (Relistor)
Uses Nalmefene (Revex)
Reversal of opioid overdose Naltrexone (ReVia, Vivitrol)
Reversal of postoperative opioid effect
Reversal of neonatal respiratory depression
Fold here
Adverse Effects
Minimal

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NONOPIOID CENTRALLY ACTING ANALGESICS NONOPIOID CENTRALLY ACTING ANALGESICS

Prototype: Tramadol (Ultram, Ultram ER) Prototype: Tramadol (Ultram, Ultram ER)
Mechanism of Action
Analog of codeine, weakly activates mu opioid receptors
Other Nonopioid Analgesics
Blocks uptake of norepinephrine and serotonin Clonidine (Duraclon)
Activates monoaminergic spinal inhibition of pain Ziconotide (Prialt)
Dexmedetomidine (Precedex)
Uses
Relieves moderate to severe pain
Fold here
Adverse Effects
Mild sedation, dizziness, headache, dry mouth, constipation
Increases the risk of seizure
Minimal respiratory depression
CNS depression if used with ETOH
HTN if used with monoamine oxidase (MAO) inhibitors
Serotonin syndrome if used with antidepressants or triptans
Low potential for abuse; not a scheduled drug

ERGOT ALKALOIDS ERGOT ALKALOIDS
Ch 30 Drugs for Headache

Prototype: Ergotamine (Ergomar) Prototype: Ergotamine (Ergomar)
Mechanism of Action
Alters transmission at serotonergic, dopaminergic,
Other Ergot Alkaloids
and alpha-adrenergic junctions Dihydroergotamine (D.H.E. 45, Migranal)
Activates serotonin receptors Ergotamine ! caffeine (Cafergot, Ercaf)
Suppresses inflammation by blocking calcitonin gene–related peptide
(CGRP)
Promotes constriction
Fold here
Uses
Migraine and cluster headaches
Adverse Effects
Nausea and vomiting
Weakness in the legs, myalgias, tingling in the fingers and toes
Angina-like pain
Tachycardia or bradycardia
Overdose can cause ergotism (ischemia due to constriction of vessels)
Fetal harm
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SEROTONIN1B/1D–RECEPTOR AGONISTS (TRIPTANS) SEROTONIN1B/1D–RECEPTOR AGONISTS (TRIPTANS)
Ch 30 Drugs for Headache

Prototype: Sumatriptan (Imitrex) Prototype: Sumatriptan (Imitrex)
Mechanism of Action
Binds to 5-HT1B/1D (serotonin) receptors to cause vasoconstriction
Other Triptans
Reduces release of inflammatory peptides (CGRT) Naratriptan (Amerge)
Diminishes perivascular inflammation Rizatriptan (Maxalt)
Relieves migraine pain and associated symptoms Zolmitriptan (Zomig)
Almotriptan (Axert)
Uses Frovatriptan (Frova)
Fold here
Migraine headache Eletriptan (Replax)

Sumatriptan ! naproxen (Treximet)
Adverse Effects
Chest symptoms (heavy arms and chest pressure)
Coronary vasospasm
Teratogenesis
Vertigo, malaise, fatigue, tingling sensation

FIRST-GENERATION (CONVENTIONAL) FIRST-GENERATION (CONVENTIONAL)
Ch 31 Antipsychotic Agents and Their Use in Schizophrenia

ANTIPSYCHOTICS ANTIPSYCHOTICS
Prototype: Chlorpromazine (Thorazine) Prototype: Chlorpromazine (Thorazine)
Mechanism of Action
Relieves positive symptoms of schizophrenia Other First-Generation Conventional Neuroleptics
Blocks receptors for dopamine (D2), acetylcholine (ACh), Low Potency
histamine, and norepinephrine (NE)
Chlorpromazine (Thorazine)
Uses Thioridazine (Mellaril)
Schizophrenia, bipolar disorder, Tourette’s syndrome
Fold here
Prevention of emesis, and dementia Medium Potency
Loxapine (Loxitane)
Adverse Effects
Molindone (Modan)
Extrapyramidal symptoms (EPS)
(acute dystonia, parkinsonism, akathisia, tardive dyskinesia) Pherphenazine
Neuroleptic malignant syndrome
(lead pipe rigidity, high fever, autonomic instability) High Potency
Anticholinergic effects (BUDCAT), orthostatic hypotension Haloperidol (Haldol), Haldol Decanoate (depot preparation)
Sedation, neuroendocrine effects, seizures Fluphenazine (Prolixin Decanoate [depot preparation])
Sexual dysfunction, increased risk of sunburn Trifluoperazine, Thiothixene (Navane)
Agranulocytosis, dysrhythmias (prolongs QT interval) Pimozide (Orap)
Counteracts the effect of levodopa used in Parkinson’s disease
Rate of mortality doubles when used in elderly patients with dementia
Increases prolactin levels Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
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SECOND-GENERATION (ATYPICAL) ANTIPSYCHOTICS SECOND-GENERATION (ATYPICAL) ANTIPSYCHOTICS
Ch 31 Antipsychotic Agents and Their Use in Schizophrenia

Prototype: Clozapine (Clozaril) Prototype: Clozapine (Clozaril)
Mechanism of Action
Relieves positive, negative, and cognitive signs and symptoms of
Other Second-Generation (Atypical) Antipsychotics
schizophrenia Risperidone (Risperdal)
Blocks receptors for serotonin (5-HT), D2, ACh, histamine, and NE Risperdal Consta (depot preparation)
Paliperidone (Invega)
Uses Olanzapine (Zyprexa)
Schizophrenia Quetiapine (Seroquel)
Fold here
Levodopa-induced psychosis Ziprasidone (Geodon)

Bipolar disorder Aripiprazole (Abilify)
Adverse Effects
Agranulocytosis
Metabolic effects (weight gain, diabetes, dyslipidemia)
Seizures, myocarditis, orthostatic hypotension
Rate of mortality doubles when used in elderly patients with dementia
Sedation, weight gain, anticholinergic effects (BUDCAT)
Lower risk of extrapyramidal effects
Costs 10 times more than conventional agents
TRICYCLIC ANTIDEPRESSANTS (TCAs) TRICYCLIC ANTIDEPRESSANTS (TCAs)
Ch 32 Antidepressants
Prototype: Imipramine (Tofranil) Prototype: Imipramine (Tofranil)
Mechanism of Action
Inhibits reuptake of norepinephrine (NE) and serotonin
Other TCAs
(more serotonin and NE are available at the synapse) Amitriptyline
Clomipramine (Anafranil)
Uses Desipramine (Norpramin)
Depression, bipolar disorder, neuropathic pain Doxepin (Sinequan)
Chronic insomnia Maprotiline
Fold here
Attention deficit/hyperactivity disorder Nortriptyline (Aventyl, Pamelor)
Panic disorder, obsessive-compulsive disorder (OCD) Protriptyline (Vivactil)
Trimipramine (Surmontil)
Adverse Effects
Orthostatic hypotension, anticholinergic effects (BUDCAT)
Diaphoresis (sweating), sedation
Cardiotoxicity, seizures, hypomania
Increased risk of suicide, especially in younger individuals
Many drug interactions
Selective serotonin reuptake inhibitors (SSRIs) preferred for treatment of
depression
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SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs) SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs)
Prototype: Fluoxetine (Prozac, Sarafem) Prototype: Fluoxetine (Prozac, Sarafem)
Mechanism of Action
Inhibits serotonin reuptake (more serotonin is available at the synapse)
Other SSRIs
Paroxetine (Paxil, Paxil CR, Pexeva)
Uses Fluvoxamine (Luvox)
Major depression, bipolar disorder Sertraline (Zoloft)
Obsessive-compulsive disorder Citalopram (Celexa)
Panic disorder, bulimia nervosa Escitalopram (Lexapro)
Fold here
Premenstrual dysphoric disorder

Adverse Effects
Sexual dysfunction, nausea, headache, insomnia
Weight gain, serotonin syndrome
Withdrawal syndrome
Neonatal abstinence syndrome and persistent pulmonary hypertension
Teratogenesis
Increased risk of suicide
Extrapyramidal side effects
Bruxism (clenching and grinding of the teeth)
Decrease in platelet aggregation, leading to bleeding
Hyponatremia
SEROTONIN/NOREPINEPHRINE REUPTAKE SEROTONIN/NOREPINEPHRINE REUPTAKE
INHIBITORS (SNRIs) INHIBITORS (SNRIs)
Prototype: Venlafaxine (Effexor) Prototype: Venlafaxine (Effexor)
Mechanism of Action
Blocks norepinephrine (NE) and 5-HT uptake; weak blockade
Other SNRIs
of dopamine uptake Duloxetine (Cymbalta)
(more transmitter available at synapse) (indicated for physical pain and diabetic neuropathy; can cause liver toxicity)
Desvenlafaxine (Pristiq)
Uses
Fold here
Major depression, generalized anxiety disorder
Social anxiety disorder (social phobia)
Adverse Effects
Nausea, headache, anorexia, nervousness, sweating, somnolence, and insomnia
Weight loss, diastolic hypertension
Sexual dysfunction, hyponatremia
Increased risk of suicide
Intense withdrawal syndrome with abrupt discontinuation
(anxiety, agitation, tremors, headache, vertigo, nausea, tachycardia, tinnitus)
Neonatal withdrawal syndrome
Serotonin syndrome
Fetal harm
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MONOAMINE OXIDASE INHIBITORS (MAOIs) MONOAMINE OXIDASE INHIBITORS (MAOIs)
Prototype: Isocarboxazid (Marplan) Prototype: Isocarboxazid (Marplan)
Mechanism of Action
Increases NE and serotonin by blocking the enzyme that inactivates them
Other MAOIs
Phenelzine (Nardil)
Uses Tranylcypromine (Parnate)
Atypical depression, bulimia nervosa, OCD, and panic attacks Transdermal selegiline (Emsam)
Adverse Effects
Fold here
CNS stimulation (anxiety, insomnia, agitation, hypomania, and mania)

Orthostatic hypotension due to vasodilation
Hypertensive crisis from high levels of dietary tyramine
Many drug interactions
SSRIs preferred for treatment of depression

ATYPICAL ANTIDEPRESSANTS ATYPICAL ANTIDEPRESSANTS
Prototype: Bupropion (Wellbutrin, Zyban) Prototype: Bupropion (Wellbutrin, Zyban)
Mechanism of Action Other Atypical Antidepressants
Unclear; may be related to blockade of dopamine uptake Nefazodone (can cause liver failure)
Mirtazapine (Remeron)
Uses Amoxapine
Major depressive disorder Reboxetine
Prevention of seasonal affective disorder (SAD) Trazodone (Desyrel) has sedative effects
Smoking cessation
Fold here
Relief of neuropathic pain (unlabeled use)
Attention deficit/hyperactivity disorder (unlabeled use)
Adverse Effects
Risk of seizure
May increase the risk of suicide
Agitation, headache, dry mouth, constipation, weight loss,
GI upset, dizziness, tremor, insomnia, blurred vision, and tachycardia

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MOOD-STABILIZING DRUGS MOOD-STABILIZING DRUGS
Ch 33 Drugs for Bipolar Disorder

Prototype: Lithium (Lithobid, Lithonate, Lithotabs) Prototype: Lithium (Lithobid, Lithonate, Lithotabs)
Mechanism of Action
Mechanism unclear; may alter ions and neurotransmitters
Other Mood-Stabilizing Drugs
May protect against neuronal atrophy and/or promote neuronal growth Antiepileptic Drugs
Valproic acid
Uses Carbamazepine
Stabilizes mood in patients with bipolar disorder Lamotrigine (Lamictal)
Reduces euphoria, hyperactivity, and other symptoms
Fold here
Preferred for patients with classic (euphoric) mania Atypical Antipsychotics

Olanzapine (Zyprexa)
Adverse Effects Aripiprazole (Abilify)
Accumulates to toxic levels in the presence of a low sodium level Ziprasidone (Geodon)
Lithium levels must be kept below 1.5 mEq/L
Blood levels are 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
FDA Pregnancy Risk Category D
Reversible leukocytosis, dermatologic reactions
Drug interactions occur with diuretics, NSAIDs, and anticholinergics Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
MOOD-STABILIZING ANTIEPILEPTIC DRUGS MOOD-STABILIZING ANTIEPILEPTIC DRUGS
Ch 33 Drugs for Bipolar Disorder

Prototype: Valproic Acid (Depakote) Prototype: Valproic Acid (Depakote)
Mechanism of Action
Suppresses mania and stabilizes mood
Other AEDs used for BPD
Carbamazepine (Equetro, Tegretol)—monitor CBC
Uses Lamotrigine (Lamictal)
Mood stabilizer for patients with bipolar disorder
Adverse Effects
Fold here
GI disturbances, weight gain
Thrombocytopenia, pancreatitis, liver failure
Target trough level is 50 to 120 mg/mL
Fetal harm

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BENZODIAZEPINES (BZDs) BENZODIAZEPINES (BZDs)
Ch 34 Sedative-Hypnotic Drugs
Prototype: Alprazolam (Xanax) Prototype: Alprazolam (Xanax)
Mechanism of Action Chlordiazepoxide (Librium)
Depresses central nervous system function Clonazepam (Klonopin)
Reduces anxiety, promotes sleep Clorazepate (Tranxene)
Potentiates the actions of GABA (an inhibitory neurotransmitter) Diazepam (Valium)
Estazolam (ProSom)
Uses Flurazepam (Dalmane)
Anxiety, insomnia, seizure disorder, induction of anesthesia Lorazepam (Ativan)
Fold here
Muscle spasm, panic disorder, and withdrawal from alcohol Midazolam (Versed)
Oxazepam (Serax)
Adverse Effects Quazepam (Doral)
CNS depression, anterograde amnesia Temazepam (Restoril)
Sleep driving and other complex sleep-related behaviors Triazolam (Halcion)
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)
BENZODIAZEPINE-LIKE DRUGS BENZODIAZEPINE-LIKE DRUGS
Prototype: Zolpidem (Ambien) Prototype: Zolpidem (Ambien)
Mechanism of Action
Potentiate the actions of GABA (an inhibitory neurotransmitter)
Other BZD-like drugs
Zaleplon (Sonata)
Uses Eszopiclone (Lunesta)
Short-term management of insomnia Melatonin Agonist
Adverse Effects Ramelteon (Rozerem)
Fold here
Daytime drowsiness, dizziness
Sleep driving and other complex sleep-related behaviors
Do not use with alcohol or other CNS depressants

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BARBITURATES BARBITURATES
CNS Depressants CNS Depressants
Mechanism of Action Thiopental
Potentiate the actions of GABA (an inhibitory neurotransmitter) Secobarbital
Phenobarbital
Uses
Insomnia
Miscellaneous Sedative-Hypnotics
Suppression of seizures, induction of general anesthesia Chloral hydrate (Aquachloral Supprettes, Somnote)
Treatment of manic states Meprobamate (Miltown)
Fold here
Paraldehyde (Paral)
Adverse Effects Trazodone (Desyrel) antidepressant
Respiratory depression, decreased blood pressure and heart rate Diphenhydramine (Sominex)
Induction of hepatic drug-metabolizing enzymes (increases the metabolism Doxylamine (Unisom)
of other drugs rendering them less effective)
May lead to tolerance and dependence
Frequently used as vehicles for suicide
Teratogenic

CNS STIMULANTS CNS STIMULANTS
Ch 36 CNS Stimulants and Attention-Deficit/Hyperactivity Disorder

Prototype: Methylphenidate Prototype: Methylphenidate
(Ritalin, Metadate, Concerta, Daytrana) (Ritalin, Metadate, Concerta, Daytrana)
Mechanism of Action
Promotes norepinephrine (NE) and dopamine (DA) release
Other CNS Stimulants
Inhibits NE and DA reuptake Dexmethylphenidate (Focalin)
Dexedrine
Uses Adderall
Attention deficit/hyperactivity disorder (ADHD) Modafinil (Provigil)
Fold here
Narcolepsy Atomoxetine (Strattera)—nonstimulant
Adverse Effects
Insomnia, reduced appetite, weight loss
Palpitations, hypertension, angina, dysrhythmias, psychosis
Abrupt discontinuation can lead to withdrawal reactions
Potential for abuse (Schedule II)
Sudden death

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DISULFIRAM (ANTABUSE) DISULFIRAM (ANTABUSE)
Ch 38 Drug Abuse II: Alcohol

Aversion Therapy for Alcoholism Aversion Therapy for Alcoholism
Mechanism of Action
Disrupts alcohol metabolism by blocking enzyme
Acetaldehyde accumulates and produces unpleasant effects
Uses
Alcohol abuse
Fold here
Adverse Effects
Nausea, vomiting, flushing, palpitations, headache
Sweating, blurry vision, hypotension, chest pain
Shock occurs with ingestion of 7 mL of alcohol

HIGH-CEILING (LOOP) DIURETICS HIGH-CEILING (LOOP) DIURETICS
Ch 40 Diuretics
Prototype: Furosemide (Lasix) Prototype: Furosemide (Lasix)
Mechanism of Action
Blocks reabsorption of sodium and chloride in the descending limb of
Other High-Ceiling Diuretics
Henle’s loop to promote urination Ethacrynic acid (Edecrin)
Produces profound diuresis Bumetanide (Bumex)
Torsemide (Demadex)
Uses
Rapid mobilization of fluid
Fold here
Pulmonary edema resulting from heart failure or renal or liver disease
Especially useful in patients with renal insufficiency
Adverse Effects
Hyponatremia, hypochloremia, dehydration, hypotension, hypokalemia
Ototoxicity, hyperglycemia, hyperuricemia, fetal harm
Raises LDL and lowers HDL (minimally)
May cause dysrhythmias when used with digoxin (reduces potassium)

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THIAZIDE DIURETICS THIAZIDE DIURETICS
Ch 40 Diuretics
Prototype: Hydrochlorothiazide (HCTZ) Prototype: Hydrochlorothiazide (HCTZ)
Mechanism of Action
Blocks reabsorption of sodium and chloride in the early segment of the distal
Other Thiazides and Related Diuretics
convoluting tubule to promote urination Chlorothiazide (Diuril)
Methyclothiazide (Enduron)
Uses Chlorthalidone (Hygroton, Thalitone)
Treatment of hypertension Metolazone (Zaroxolyn)
Mobilization of edema with mild heart failure, hepatic or renal disease
Fold here
Ineffective when GFR is low ("15 to 20 mL/min)

Adverse Effects
Hyponatremia, hypochloremia, dehydration
Hypokalemia, magnesium deficiency, and hypotension
Hyperglycemia, hyperuricemia, increase in LDL and triglycerides
May cause dysrhythmias when used with digoxin (reduces potassium)
Fetal harm

POTASSIUM-SPARING DIURETICS POTASSIUM-SPARING DIURETICS
Ch 40 Diuretics
Prototype: Spironolactone (Aldactone) Prototype: Spironolactone (Aldactone)
Mechanism of Action
Blocks the actions of aldosterone in the distal nephron
Other Potassium-Sparing Diuretics
Produces minimal diuresis Triamterene (Dyrenium)
Causes retention of potassium and increased excretion of sodium Amiloride (Midamor)
Uses Other Aldosterone Blockers

Hypertension and edema Eplerenone (Inspra)
Fold here
Used in combination with other diuretics to counterbalance potassium loss Not considered a diuretic
Heart failure Used for heart failure
(Blocks the negative effects of aldosterone on the heart and blood vessels)
Primary hyperaldosteronism, premenstrual syndrome
Polycystic ovary syndrome, and acne
Adverse Effects
Hyperkalemia, dysrhythmias
Endocrine effects
(Gynecomastia, menstrual irregularities, impotence, and hirsutism)

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OSMOTIC DIURETICS OSMOTIC DIURETICS
Ch 40 Diuretics
Prototype: Mannitol (Osmitrol) Prototype: Mannitol (Osmitrol)
Mechanism of Action
Creates an osmotic force in the lumen of the nephron
Promotes diuresis by inhibiting passive reabsorption of water
Uses
Prophylaxis of renal failure
Reduction of intracranial pressure
Fold here
Reduction of intraocular pressure

Adverse Effects
Edema
CHF and pulmonary edema

ANGIOTENSIN-CONVERTING ENZYME (ACE) ANGIOTENSIN-CONVERTING ENZYME (ACE)
Ch 43 Drugs Acting on the Renin-Angiotensin-Aldosterone System

INHIBITORS INHIBITORS
Prototype: Ramipril (Altace) Prototype: Ramipril (Altace)
Mechanism of Action
Inhibits ACE, reducing levels of angiotensin II
Other ACE Inhibitors
Dilates arterioles and veins to reduce blood volume and BP Benazepril (Lotensin)
Prevents pathologic changes in cardiac structure Captopril (Capoten)
Enalapril (Vasotec)
Uses Fosinopril (Monopril)
Fold here
Hypertension, heart failure, MI Lisinopril (Prinivil and Zestril)
Diabetic and nondiabetic nephropathy Moexipril (Univasc)
Prevention of MI, stroke, and death Perindopril (Aceon)
Quinapril (Accupril)
Adverse Effects Trandolapril (Mavik)
Hypotension, cough, hyperkalemia
Renal failure in patients with renal artery stenosis
Fetal injury
Angioedema
Neutropenia, dysgeusia, and rash with captopril

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ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs) ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs)

Prototype: Losartan (Diovan) Prototype: Losartan (Diovan)
Mechanism of Action
Blocks the action of angiotensin II
Other ARBs
Dilates arterioles and veins to reduce blood volume and BP Candesartan (Atacand)
Prevents pathologic changes in cardiac structure Eprosartan (Teveten)
Does not cause cough or significant hyperkalemia Irbesartan (Avalide)
Losartan (Hyzaar)
Uses Olmesartan (Benicar)
Fold here
Hypertension, heart failure, MI, and diabetic nephropathy Telmisartan (Micardis)

Prevention of MI, stroke, and death
Adverse Effects
Renal failure in patients with renal artery stenosis
Hypotension
Angioedema
Fetal harm

DIRECT RENIN INHIBITORS (DRIs) DIRECT RENIN INHIBITORS (DRIs)

Prototype: Aliskiren (Tekturna) Prototype: Aliskiren (Tekturna)
Mechanism of Action
Binds with renin and inhibits the formation of angiotensin I
Uses
Hypertension
Adverse Effects
Fold here
Angioedema and cough
GI effects (diarrhea)
Hyperkalemia
Fetal injury and death

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ALDOSTERONE ANTAGONISTS ALDOSTERONE ANTAGONISTS

Prototype: Eplerenone (Inspra) Prototype: Eplerenone (Inspra)
Mechanism of Action
Blocks aldosterone, increases excretion of sodium and water
Other Aldosterone Antagonists
Retention of potassium Spironolactone
Reduces blood volume and blood pressure
Prevents cardiovascular remodeling
Uses
Fold here
Hypertension, heart failure
Adverse Effects
Hyperkalemia

CALCIUM CHANNEL BLOCKERS CALCIUM CHANNEL BLOCKERS
Ch 44 Calcium Channel Blockers

Nondihydropyridines Nondihydropyridines
Prototypes: Verapamil (Calan) and Diltiazem Prototypes: Verapamil (Calan) and Diltiazem
(Cardizem) (Cardizem)
Mechanism of Action
Block calcium channels in the heart and blood vessels
Dilate peripheral arterioles to reduce blood pressure
Increase coronary perfusion
Fold here
Block SA and AV nodes to reduce heart rate and contractility
Reduce force of myocardial contraction
Uses
Angina, essential hypertension, cardiac dysrhythmias
Adverse Effects
Constipation, dizziness, facial flushing, peripheral edema, hypotension
Bradycardia, AV block, decreased cardiac contractility
Chronic eczematous rash and gingival hyperplasia
Verapamil increases digoxin level by 60%
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CALCIUM CHANNEL BLOCKERS CALCIUM CHANNEL BLOCKERS
Ch 44 Calcium Channel Blockers

Dihydropyridine Dihydropyridine
Prototype: Amlodipine (Norvasc) Prototype: Amlodipine (Norvasc)
Mechanism of Action
Blocks calcium channels in the blood vessels
Other Dihydropyridine Calcium Channel Blockers
Little effect on heart rate or contractility Nifedipine (Adalat, Procardia)
Vasodilation in peripheral arterioles lowers blood pressure Nicardipine (Cardene)
Calcium channel blockade in coronary arteries increases perfusion Isradipine (DynaCirc)
Fold here
Felodipine (Plendil)
Uses Nimodipine (Nimotop)
Hypertension Nisoldipine (Sular)
Angina
Adverse Effects
Hypotension, edema, flushing, dizziness, headache
Peripheral edema, gingival hyperplasia, chronic eczematous rash
Does not slow heart rate, as do verapamil and diltiazem

VASODILATORS VASODILATORS
Ch 45 Vasodilators
Prototype: Hydralazine (Apresoline) Prototype: Hydralazine (Apresoline)
Mechanism of Action
Selective dilation of arterioles (mechanism unknown)
Other Vasodilators
Decrease in peripheral resistance and arterial blood pressure BiDil (hydralazine and isosorbide dinitrate)
Increase in heart rate and myocardial contractility by reflex Minoxidil
Diazoxide (Hyperstat IV)
Uses Sodium nitroprusside (Nitropress)
Essential hypertension, hypertensive crisis, heart failure Angiotensin-converting enzymes (ACE) inhibitors
Fold here
Angiotensin II receptor blockers (ARBs)
Adverse Effects Direct renin inhibitors (DRIs)
Calcium channel blockers (CCBs)
Reflex tachycardia
Alpha-adrenergic blocking agents
Increased blood volume
Ganglionic blocking agents
Systemic lupus erythematosus–like syndrome
Adrenergic neuron blocking agents
Headache, dizziness, weakness, and fatigue
Centrally acting alpha2 agonists
Nesiritide (Natrecor)
Drugs used for pulmonary artery hypertension

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CARDIAC (DIGITALIS) GLYCOSIDES CARDIAC (DIGITALIS) GLYCOSIDES
Ch 47 Drugs for Heart Failure

Prototype: Digoxin (Lanoxin) Prototype: Digoxin (Lanoxin)
Positive Inotropic Agent for Heart Failure Positive Inotropic Agent for Heart Failure
Mechanism of Action
Increases the force of ventricular contraction to increase cardiac output Other Drugs Used to Treat Heart Failure
Inhibits Na!, K!-ATPase to increase Ca!! inside myocytes Diuretics
Competes with K! for binding to Na!, K!-ATPase ACE inhibitors
↓ K → ↑ Na!, K!-ATPase inhibition → digoxin toxicity
Angiotensin receptor blockers
Changes electrical activity of heart and slows heart rate
Fold here
Increased cardiac output → decreased sympathetic tone, increased urine production, Beta blockers
and decreased release of renin Aldosterone blockers
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 Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
CLASS I: SODIUM CHANNEL BLOCKERS CLASS I: SODIUM CHANNEL BLOCKERS
Ch 48 Antidysrhythmic Drugs
Prototype: Procainamide (Procanbid) Prototype: Procainamide (Procanbid)
Class IA Sodium Channel Blocker Class IA Sodium Channel Blocker
Mechanism of Action
Blocks cardiac sodium channels
Other Class IA Sodium Channel Blockers
Slows conduction in the atria, ventricles, and His-Purkinje system Quinidine
Delays depolarization Disopyramide (Norpace)
Fold here
Uses
Atrial and ventricular dysrhythmias
Adverse Effects
Systemic lupus erythematosus–like syndrome
Blood dyscrasias
QRS widening and prolongation

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CLASS I: SODIUM CHANNEL BLOCKERS CLASS I: SODIUM CHANNEL BLOCKERS
Class IB Sodium Channel Blocker Class IB Sodium Channel Blocker
Prototype: Lidocaine (Xylocaine) Prototype: Lidocaine (Xylocaine)
Mechanism of Action
Blocks cardiac sodium channels
Other Sodium Channel–Blocking Antidysrhythmics
Slows conduction in the atria, ventricles, and His-Purkinje system Class IB
Reduces automaticity in the ventricles and His-Purkinje system Mexiletine (Mexitil)
Accelerates repolarization Phenytoin (Dilantin)
Fold here
Uses Class IC
Short-term therapy for ventricular dysrhythmias Flecainide (Tambocor)
Propafenone (Rythmol)
Adverse Effects
No significant impact on the ECG Other Class I
Drowsiness, confusion, and paresthesias Moricizine (Ethmozine)
Toxic doses may produce convulsions and respiratory arrest

CLASS II: BETA BLOCKERS CLASS II: BETA BLOCKERS
Prototype: Propranolol (Inderal) Prototype: Propranolol (Inderal)
Mechanism of Action
Nonselective beta-adrenergic antagonist
Other Class II Agents
Attenuates sympathetic stimulation of the heart Acebutolol (Sectral)
Blocks both beta1 and beta2 receptors Esmolol (Brevibloc)
Reduces automaticity of the SA node
Reduces velocity of conduction through the AV node (prolongs PR interval)
Reduces myocardial contractility
Fold here
Uses
Sinus tachycardia, severe recurrent ventricular tachycardia
Exercise-induced tachydysrhythmias
Paroxysmal atrial tachycardia provoked by emotion or exercise
Angina of effort
Adverse Effects
Prolongs PR interval on the ECG
Bradycardia, heart failure, AV block, and sinus arrest
Hypotension, bronchospasm in patients with asthma
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CLASS III: POTASSIUM CHANNEL BLOCKERS CLASS III: POTASSIUM CHANNEL BLOCKERS
Prototype: Amiodarone (Cordarone, Pacerone) Prototype: Amiodarone (Cordarone, Pacerone)
Mechanism of Action
Delays repolarization Other Class III Agents
Reduces automaticity in the SA node, reduces contractility Bretylium
Reduces conduction velocity in the AV node, ventricles, and His-Purkinje system Sotalol (Betapace) class II and class III
Dilates coronary and peripheral blood vessels Dofetilide (Tikosyn)
Ibutilide (Corvert)
Uses
Recurrent ventricular fibrillation
Fold here
Unstable ventricular tachycardia
Adverse Effects
Pulmonary toxicities (pneumonitis and fibrosis)
Widening of the QRS complex, prolongation of the PR and QT intervals
Sinus bradycardia, AV block, precipitation of heart failure, hypotension
Toxicities in pregnancy
Corneal microdeposits, optic neuropathy
Blue-gray discoloration of the skin
GI reactions (anorexia, nausea, vomiting)
CNS reactions (ataxia, dizziness, tremor, mood alterations, hallucinations)
Hepatitis, thyroid dysfunction
Grapefruit juice increases levels to toxicity Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
CLASS IV: CALCIUM CHANNEL BLOCKERS CLASS IV: CALCIUM CHANNEL BLOCKERS
Prototypes: Verapamil (Calan, Isoptin, Verelan) Prototypes: Verapamil (Calan, Isoptin, Verelan)
Diltiazem (Cardizem, others) Diltiazem (Cardizem, others)
Mechanism of Action
Block calcium channels in the heart
Other Antidysrhythmic Drugs
Slow SA node automaticity, delay AV node conduction Adenosine (Adenocard)
Reduce myocardial contractility Digoxin (Lanoxin)
Uses
Fold here
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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HMG-CoA REDUCTASE INHIBITORS (STATINS) HMG-CoA REDUCTASE INHIBITORS (STATINS)
Ch 49 Prophylaxis of Coronary Heart Disease

Prototype: Atorvastatin (Lipitor) Prototype: Atorvastatin (Lipitor)
Mechanism of Action
Inhibits the enzyme (HMG-CoA) that synthesizes cholesterol Other “Statins”
Increases the number of LDL receptors on liver cells to remove more LDL
Decreases production of VLDLs and raises HDL levels Fluvastatin (Lescol)
Stabilizes plaque, slows progression of coronary calcification Lovastatin (Mevacor, Altoprev)
Improves endothelial function Pravastatin (Pravachol)
Enhances the ability of blood vessels to dilate
Reduces the risk of thrombosis
Rosuvastatin (Crestor)
Inhibits platelet deposition and aggregation Simvastatin (Zocor)
Fold here
May increase bone formation Cholestin (dietary supplement made from red yeast)
Uses
Hypercholesterolemia
Primary and secondary prevention of CV events
Post MI therapy
Prevention of CV events in people with diabetes
Adverse Effects
Headache, rash, GI complaints
Myopathy, increases CK levels, rhabdomyolysis, dark urine, renal failure
Hepatotoxicity, increases ALT and AST
Rare peripheral neuropathy
FDA Pregnancy risk Category X
Drug Interactions
Macrolide antibiotics, azole antifungals
HIV protease inhibitors, amiodarone, cyclosporine, and grapefruit juice raise some Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
statins to toxic levels
NICOTINIC ACID NICOTINIC ACID

Prototype: Nicotinic Acid (Niacor, Niaspan) Prototype: Nicotinic Acid (Niacor, Niaspan)
Mechanism of Action
Reduces LDL and triglycerides
Drug Combinations
Increases HDL Lovastatin/niacin (Advicor)
Simvastatin/niacin (Simcor)
Uses
Lowers triglycerides in patients at risk for pancreatitis
Dyslipidemia
Fold here
Reduces the risk of major coronary events
Reduces total mortality
Adverse Effects
Flushing and itching (take 325 mg ASA 30 minutes before dose)
Gastric upset, nausea, vomiting, diarrhea
Hepatotoxicity
May raise blood sugar in patients with diabetes
May increase incidence of gout

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BILE-ACID SEQUESTRANTS BILE-ACID SEQUESTRANTS

Prototype: Colesevelam (WelChol) Prototype: Colesevelam (WelChol)
Mechanism of Action
Binds (sequesters) bile acids in the GI tract
Other Agents
Prevents the absorption and promotes their excretion Cholestyramine (Questran)
Forms insoluble complex with bile acids Colestipol (Colestid)
Increases LDL receptors
Safest of all lipid-lowering drugs
Fold here
Uses
Often used in combination with statin
Approved to control hyperglycemia in patients with type 2 diabetes
Adverse Effects
Constipation, bloating, indigestion
Interferes with absorption of other drugs
May impede absorption of fat-soluble vitamins

EZETIMIBE (ZETIA) EZETIMIBE (ZETIA)

Cholesterol-Lowering Drug Cholesterol-Lowering Drug
Mechanism of Action
Inhibits cholesterol absorption in the small intestine
Drug Combinations
Reduces LDL, triglycerides, and apolipoprotein B Simvastatin/ezetimibe (Vytorin)
Small increase in HDL
Uses
Fold here
Used in combination with statins
Adverse Effects
Reports of myopathy, rhabdomyolysis, pancreatitis, and thrombocytopenia
May increase risk of liver damage when used with statins

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FIBRIC ACID DERIVATIVES (FIBRATES) FIBRIC ACID DERIVATIVES (FIBRATES)

Prototype: Gemfibrozil (Lopid) Prototype: Gemfibrozil (Lopid)
Mechanism of Action
Reduces triglycerides by lowering VLDL
Other Fibric Acid Derivatives
Raises HDL levels Fenofibrate (TriCor, Antara, Lofibra, Triglide)
Fenofibric acid (TriLipix)—approved for use with statins
Uses
Hypertriglyceridemia
Fold here
Adverse Effects
Rash, nausea, abdominal pain, diarrhea
Gallstone formation
Myopathy, liver injury
Increases warfarin levels, leading to hemorrhage
Do not combine gemfibrozil with statins

ORGANIC NITRATES (ANTIAGINAL AGENTS) ORGANIC NITRATES (ANTIANGINAL AGENTS)
Ch 50 Drugs for Angina Pectoris

Prototype: Nitroglycerin Prototype: Nitroglycerin
Mechanism of Action
Dilates veins, decreases venous return to the heart
Similar Agents
Reduces ventricular filling and wall tension (preload) Isosorbide mononitrate
Reduces cardiac oxygen demand Isosorbide dinitrate
Amyl nitrite
Uses
Angina, myocardial infarction
Other Antianginal Agents
Fold here
Beta blockers
Adverse Effects Calcium blockers
Headache, orthostatic hypotension Ranolazine (Ranexa)
Reflex tachycardia
Tolerance to drug effect
Vasospasm if withdrawn abruptly
Use with sildenafil (Viagra), other drugs for erectile dysfunction may
lead to severe hypotension

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ANTICOAGULANTS ANTICOAGULANTS
Ch 51 Anticoagulant, Antiplatelet, and Thrombolytic Drugs

Prototype: Heparin Prototype: Heparin
Mechanism of Action
Suppresses the formation of fibrin in veins Low-Molecular-Weight Heparins (LMWH)
Inactivates clotting factors thrombin and Xa Enoxaparin (Lovenox)
Anticoagulant effect develops quickly Dalteparin (Fragmin)
Tinzaparin (Innohep)
Uses LMWH can be given on a fixed dose; does not require aPTT monitoring
Used for pulmonary embolism, evolving stroke, DVT
Open heart surgery, renal dialysis
Selective Factor Xa Inhibitors
Fold here
Prevention of postoperative thrombosis

Disseminated intravascular coagulation Fondaparinux (Arixtra)
Acute myocardial infarction Rivaroxaban (Xarelto)
Monitor Direct Thrombin Inhibitors
Activated partial thromboplastin time (aPTT)
Normal aPTT: 40 seconds; therapeutic level: 60 to 80 seconds Bivalirudin (Angiomax)
Lepirudin (Refludan)
Adverse Effects Argatroban
Bleeding—antidote is protamine sulfate Desirudin (Ipravask)
Heparin-induced thrombocytopenia (HIT)
Decreased platelet count ("100,000/mm3) leads to thrombosis
Hypersensitivity reaction (fever, chills, urticaria)
May be used during pregnancy Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
ANTICOAGULANT ANTICOAGULANT

Prototype: Warfarin (Coumadin, Jantoven) Prototype: Warfarin (Coumadin, Jantoven)
Mechanism of Action
Suppresses coagulation by reducing production of clotting factors Oral Anticoagulant
Antagonizes vitamin K
Inhibits vitamin K–dependent clotting factors
Blocks synthesis of factors VII, IX, X, and prothrombin
Effect takes a few days
Uses
Long-term prophylaxis of venous thrombosis and pulmonary embolism
Fold here
Prevention of thromboembolism in patients with mechanical heart valves
Prevention of thrombosis in patients with atrial fibrillation
Prevention of transient ischemic attacks and recurrent MI
Monitor
Prothrombin time (PT)—reported as INR
Goal INR for atrial fibrillation: 2-3
Goal INR for mechanical valves: 3-4.5
Adverse Effects
Hemorrhage—antidote is vitamin K (phytonadione)
Skin disorders, GI disturbances, red-orange color of urine
Increased risk of fractures with long-term use
Many drug-drug interactions
Keep intake of vitamin K foods constant
Fetal harm Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
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ANTIPLATELET DRUGS ANTIPLATELET DRUGS

Prototype: Aspirin Prototype: Aspirin
Mechanism of Action
Irreversible inhibition of COX-1 and COX-2
Suppresses platelet aggregation
Decreases prostaglandin synthesis
Reduces the risk of arterial thrombosis
Reduces inflammation, pain, and fever
Uses
Fold here
Ischemic stroke, transient ischemic attacks (TIAs)

Chronic stable angina, unstable angina
Coronary stenting, acute MI, previous MI
Primary prevention of MI
Adverse Effects
Gastric distress (heartburn and nausea)
GI bleeding, gastric ulceration and perforation
Not used in children because of the risk of Reye’s syndrome
Fetal harm (prolongs labor, premature closure of the patent ductus)
Salicylism (tinnitus, sweating, headache, dizziness)
Hypersensitivity in patients with allergies
Renal impairment Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
Bleeding

ADENOSINE DIPHOSPHATE RECEPTOR (ADP) ADENOSINE DIPHOSPHATE RECEPTOR (ADP)
ANTAGONISTS ANTAGONISTS
Prototype: Clopidogrel (Plavix) Prototype: Clopidogrel (Plavix)
Mechanism of Action
Blocks ADP receptors so that platelets are unable to aggregate
Other, Similar Agent
Ticlopidine (Ticlid)—major adverse effects
Uses
Prevents blockage of coronary artery stints
Fold here
Reduces thrombotic events—MI, ischemic stroke, vascular death
Adverse Effects
Dyspepsia, diarrhea, rash
Intracranial hemorrhage, GI bleeding
Rare thrombotic thrombocytopenia (TTP)

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GLYCOPROTEIN llb/llla–RECEPTOR ANTAGONISTS GLYCOPROTEIN llb/llla–RECEPTOR ANTAGONISTS
Prototype: Abciximab (RePro) Prototype: Abciximab (RePro)
Mechanism of Action
Causes reversible blockade of platelet GP IIb/IIIa receptors
Other, Similar Agents
Interferes with the final step in platelet aggregation Eptifibatide (Integrilin)
Tirofiban (Aggrastat)
Uses Dipyridamole (Persantine)
Prevents ischemic events in patients with acute coronary syndrome Cilostazol (Pletal)
Fold here
Used during percutaneous angioplasty
Adverse Effects
Hemorrhage

THROMBOLYTIC DRUGS THROMBOLYTIC DRUGS

Prototype: Alteplase (tPA) Prototype: Alteplase (tPA)
Mechanism of Action
Converts plasminogen to plasmin
Plasmin is an enzyme that digests the fibrin matrix of clots Streptokinase (Streptase)
Dissolves existing thrombi Tenecteplase (TNKase)
Does not prevent thrombi from forming Reteplase (Retavase)
Urokinase (Abbokinase)
Uses
Fold here
Acute myocardial infarction, pulmonary embolism, and ischemic stroke
Adverse Effects
Bleeding
Intracranial hemorrhage

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FERROUS SULFATE FERROUS SULFATE
Ch 54 Drugs for Deficiency Anemias

Oral Iron Preparation Oral Iron Preparation
Mechanism of Action
Essential to the function of hemoglobin and myoglobin
Other Oral Iron Preparations
(oxygen-storing molecule of muscle) Ferrous fumarate
Ferrous gluconate
Uses Carbonyl iron
Iron deficiency anemia (microcytic hypochromic anemia)
Fold here
Adverse Effects
Nausea, heartburn (pyrosis), bloating, constipation, diarrhea
May turn stool dark green or black
Liquid iron preparation stains teeth
Toxic to children (lethal dose is 2 to 10 grams)

CYANOCOBALAMIN (VITAMIN B12) CYANOCOBALAMIN (VITAMIN B12)

Mechanism of Action
Essential for synthesis of DNA
Catalyzes conversion of folic acid to its active form
Uses
B12 deficiency, pernicious anemia
Macrocytic normochromic anemia (megaloblastic anemia)
Adverse Effects
Fold here
Hypokalemia
Never given IV
Folic acid can mask the hematologic effects of B12 deficiency

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FOLIC ACID (FOLATE) FOLIC ACID (FOLATE)

Mechanism of Action
Essential for synthesis of DNA
Uses
Treatment of folic acid deficiency (megaloblastic anemia)
Used prophylactically to prevent neural tube defects (NTDs)
Adverse Effects
Fold here
Does not correct neurologic consequences

Can correct anemia but may mask B12 deficiency
Always give folic acid with B12

ERYTHROPOIETIC GROWTH FACTORS ERYTHROPOIETIC GROWTH FACTORS
Ch 55 Hematopoietic Growth Factors

Prototype: Epoetin Alfa Prototype: Epoetin Alfa
(Erythropoietin, Epogen, Procrit) (Erythropoietin, Epogen, Procrit)
Mechanism of Action
Stimulates production of red blood cells in the bone marrow
Other Erythropoietic Growth Factors
Darbepoetin Alpha (Aranesp)—long acting
Uses Methoxy polyethylene glycol (Mircera)
Anemia of chronic renal failure
Anemia due to AIDS treatment with AZT (zidovudine)
Fold here
Anemia caused by chemotherapy
Anemia in patients facing surgery
Adverse Effects
Hypertension
Increase in cardiovascular events (heart failure, thrombosis, stroke and MI)
Hemoglobin level should not exceed 12 g/dL
Rise in hemoglobin should not exceed 1 g/dL in 2 weeks
Red cell aplasia (anemia due to autoimmune response)

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LEUKOPOIETIC GROWTH FACTORS LEUKOPOIETIC GROWTH FACTORS

Prototype: Filgrastim (Neupogen) Prototype: Filgrastim (Neupogen)
Mechanism of Action
Acts on bone marrow to increase production of neutrophils
Other Leukopoietic Growth Factors
Pegfilgrastim (Neulasta)
Uses Sargramostim (Leukine)
Patients undergoing myelosuppressive chemotherapy
Patients undergoing bone marrow transplantation
Harvesting of peripheral blood progenitor cells
Fold here
Severe chronic neutropenia

Reduces risk of infection
Adverse Effects
Bone pain, leukocytosis
Elevates uric acid levels, LDH, and alkaline phosphatase
Splenomegaly

THROMBOPOIETIC GROWTH FACTORS THROMBOPOIETIC GROWTH FACTORS

Prototype: Oprelvekin (Neumega) Prototype: Oprelvekin (Neumega)
Mechanism of Action
Stimulates production of platelets (thrombocytes)
Uses
Patients undergoing myelosuppressive chemotherapy
Increases platelets to minimize thrombocytopenia
Fold here
Adverse Effects
Retention of sodium and water by kidneys
Peripheral edema
Tachycardia, atrial fibrillation, atrial flutter
Severe allergic reactions
Conjunctival injection

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ORAL AGENTS FOR TYPE 2 DIABETES ORAL AGENTS FOR TYPE 2 DIABETES
Ch 56 Drugs for Diabetes Mellitus

BIGUANIDES BIGUANIDES
Prototype: Metformin Prototype: Metformin
(Glucophage, Fortamet, Glumetza, Riomet) (Glucophage, Fortamet, Glumetza, Riomet)
Mechanism of Action
Inhibits glucose production in the liver (gluconeogenesis)
Inhibits glucose absorption in the intestines
Sensitizes insulin receptors on fat and skeletal muscle
Enhances glucose uptake and metabolism by muscle
Fold here
Lowers basal and postprandial blood sugar
Uses
Type 2 diabetes
Prevention of type 2 diabetes
Treatment of polycystic ovary syndrome (PCOS)
Adverse Effects
Decreased appetite, nausea, diarrhea, and weight loss
Rare cases of lactic acidosis
Avoid in patients with renal disease (Cr #1.4 mg/dL)
Avoid in patients with ethyl alcohol (ETOH) abuse, infection, liver disease, or CHF
Discontinue 48 hours prior to test with contrast medium to avoid lactic acidosis
Can reduce vitamin B12 and folic acid absorption Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

SULFONYLUREAS SULFONYLUREAS
Prototype: Glipizide (Glucotrol, Glucotrol ER) Prototype: Glipizide (Glucotrol, Glucotrol ER)
Mechanism of Action
Stimulates insulin release from the pancreas
Other Sulfonylureas
Glyburide (DiaBeta, Micronase)
Uses Glimepiride (Amaryl)
Type 2 diabetes
Fold here
Adverse Effects
Hypoglycemia
Possible increased risk of sudden cardiac death
Fetal harm
Disulfiram-like reaction when taken with ETOH

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MEGLITINIDES MEGLITINIDES
Prototype: Repaglinide (Prandin) Prototype: Repaglinide (Prandin)
Mechanism of Action
Stimulates pancreatic insulin release
Other Meglitinide
Nateglinide (Starlix)
Uses
Type 2 diabetes
Fold here
Adverse Effects
Hypoglycemia
Administer 30 minutes before a meal


THIAZOLIDINEDIONES (GLITAZONES, TZDs) THIAZOLIDINEDIONES (GLITAZONES, TZDs)
Prototype: Rosiglitazone (Avandia) Prototype: Rosiglitazone (Avandia)
Mechanism of Action
Increases insulin sensitivity
Other TZDs
Pioglitazone (Actos)
Uses
Type 2 diabetes
Fold here
Adverse Effects
Mild headache and upper respiratory infections
Raises LDL levels
Fluid retention—caution in patients with CHF
Hepatotoxicity—monitor ALT
May increase cardiovascular events

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ALPHA-GLUCOSIDASE INHIBITORS ALPHA-GLUCOSIDASE INHIBITORS
Prototype: Acarbose (Precose) Prototype: Acarbose (Precose)
Mechanism of Action
Delays absorption of carbohydrates
Other Alpha-Glucosidase Inhibitor
Lowers postprandial blood glucose levels Miglitol (Glyset)
Uses
Type 2 diabetes
Fold here
Adverse Effects
Flatulence, cramps, abdominal distention, and diarrhea
Hypoglycemia, liver dysfunction


GLIPTINS GLIPTINS
Prototype: Sitagliptin (Januvia) Prototype: Sitagliptin (Januvia)
Mechanism of Action
Increases the incretin system
Inhibits the enzyme DPP-4, which breaks down incretin hormones
Suppresses glucagon release from the alpha cells of the pancreas
Stimulates insulin release from the beta cells of the pancreas
Turns off glucose production in the liver
Fold here
Uses
Type 2 diabetes
Adverse Effects
Nasal inflammation, upper respiratory tract infection
Minimal hypoglycemia

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NEW INJECTABLE DRUGS FOR DIABETES NEW INJECTABLE DRUGS FOR DIABETES

INCRETIN MIMETIC INCRETIN MIMETIC
Prototype: Exenatide (Byetta) Prototype: Exenatide (Byetta)
Mechanism of Action
Action similar to natural incretins released in the GI tract
Slows gastric emptying
Stimulates glucose-dependent release of insulin
Inhibits postprandial release of glucagon
Suppresses appetite
Fold here
Decreases postprandial blood glucose

Uses
Type 2 diabetes
Adverse Effects
Hypoglycemia
Nausea, vomiting, and diarrhea
Rare incidences of pancreatitis
Weight loss

NEW INJECTABLE DRUGS FOR DIABETES NEW INJECTABLE DRUGS FOR DIABETES

AMYLIN MIMETIC AMYLIN MIMETIC
Prototype: Pramlintide (Symlin) Prototype: Pramlintide (Symlin)
Mechanism of Action
Mimics the effects of amylin (hormone made in the pancreas)
Reduces postprandial levels of glucose
Delays gastric emptying
Suppresses glucagon secretion
Increases the sense of satiety
Fold here
Enhances the effects of mealtime insulin
Uses
Type 1 and type 2 diabetes
Adverse Effects
Hypoglycemia when combined with other agents
Nausea
Injection site reactions

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INJECTABLE DRUGS FOR DIABETES INJECTABLE DRUGS FOR DIABETES

GLUCAGON GLUCAGON
Mechanism of Action
Hormone that increases plasma levels of glucose
Opposite effect of insulin
Uses
Treats hypoglycemia from insulin overdose
Used only if intravenous glucose is not available
Fold here
Adverse Effects
Nausea and vomiting
Place patient on side after administration

THYROID HORMONES THYROID HORMONES
Ch 57 Drugs for Thyroid Disorders

Prototype: Levothyroxine (Synthroid, Levoxyl) Prototype: Levothyroxine (Synthroid, Levoxyl)
Synthetic Preparation of T4 Synthetic Preparation of T4
Mechanism of Action
Converted to T3 in the body
Other Thyroid Hormone Preparations
Thyroid hormone replacement Liothyronine (Cytomel, Triostat) T3
Liotrix (Thyrolar) T3, T4 combination
Uses Armour Thyroid—desiccated animal thyroid glands
Fold here
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
Take on an empty stomach
Do not mix with calcium or iron

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ANTITHYROID DRUGS ANTITHYROID DRUGS
Ch 57 Drugs for Thyroid Disorders

Prototype: Propylthiouracil (PTU) Prototype: Propylthiouracil (PTU)
Mechanism of Action
Inhibits thyroid hormone synthesis
Other Antithyroid Drugs
Inhibits conversion of T4 to T3 in the periphery Methimazole (Tapazole)
Radioactive iodine (131I)
Uses Nonradioactive iodine—(Lugol’s solution)
Hyperthyroidism, Graves’ disease Sodium iodide (IV)
Thyrotoxic crisis Potassium iodide (Thyro-Block)
Fold here
Propranolol (Inderal) suppresses tachycardia

Adverse Effects
Agranulocytosis, hypothyroidism
Fetal harm, rash, nausea, arthralgia, headache
Dizziness, paresthesias, and liver injury
May take 6 to 12 months to develop

ERECTILE DYSFUNCTION DRUGS ERECTILE DYSFUNCTION DRUGS
Ch 65 Drugs for Erectile Dysfunction and Benign Prostatic Hyperplasia

PDE-5 Inhibitors PDE-5 Inhibitors
Prototype: Sildenafil (Viagra) Prototype: Sildenafil (Viagra)
Mechanism of Action
Enhances the normal erectile response to sexual stimuli by inhibiting PDE-5
Other Erectile Dysfunction Drugs
Tadalafil (Cialis)
Uses Vardenafil (Levitra)
Erectile dysfunction Papaverine plus phentolamine injection
Fold here
Alprostadil (prostaglandin E1)
Adverse Effects
Hypotension, priapism
Nonarteritic ischemic optic neuropathy (NAION)
Sudden hearing loss, dizziness, vertigo, tinnitus
Headache, flushing, dyspepsia, nasal congestion
Visual changes (blue color tinge, light sensitivity, blurring)
Use with nitrates and alpha blockers leads to hypotension

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DRUGS FOR BENIGN PROSTATIC HYPERTROPHY (BPH) DRUGS FOR BENIGN PROSTATIC HYPERTROPHY (BPH)
Ch 65 Drugs for Erectile Dysfunction and Benign Prostatic Hyperplasia

5-alpha-Reductase Inhibitors 5-alpha-Reductase Inhibitors
Prototype: Finasteride (Proscar) Prototype: Finasteride (Proscar)
Mechanism of Action
Reduces levels of dihydrotestosterone (DHT)
Other 5-alpha Reductase Inhibitor
Promotes regression of prostate epithelial tissue Dutasteride (Avodart)
Reduces mechanical obstruction of the urethra
Alpha1-Adrenergic Antagonists
Fold here
Adverse Effects Terazosin (Hytrin)

Reduces ejaculate volume and libido Doxazosin (Cardura)
Gynecomastia (breast enlargement) Tamsulosin (Flomax)—used for BPH only
Reduces prostate-specific antigen (PSA) Alfuzosin (Uroxatral)—used for BPH only
May mask an elevated PSA
Benefits develop slowly over 6 to 12 months
Other Drugs for BPH
Saw palmetto
Tolterodine (Detrol)
PDE-5 inhibitors
Botox

LIVE VIRUS VACCINES LIVE VIRUS VACCINES
Ch 67 Childhood Immunization
Live virus vaccines are contraindicated in pregnancy Varicella (Varivax)
Give with caution in immunocompromised patients
Oral Polio Vaccine (OPV) not used in the
United States
Measles, Mumps, and Rubella Virus Vaccine (MMR)
Live Influenza Attenuated Vaccine (LIAV)
Fold here
Yellow fewer vaccine
Zoster vaccine (Zostavax)
Rotavirus vaccine (Rotarix, Rota Teq)

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IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS
Ch 68 Immunosuppressants
Prototype: Cyclosporine Prototype: Cyclosporine
(Sandimmune, Gengraf, Neoral) (Sandimmune, Gengraf, Neoral)
Mechanism of Action
Suppresses production of inflammatory cells
Other Immunosuppressants
Reduces B cells and cytotoxic T cells Tacrolimus (Prograf)
Sirolimus (Rapamune)
Uses Glucocorticoids
Prevents rejection of organ transplants Cytotoxic drugs
Fold here
Antibodies
Adverse Effects
Nephrotoxicity, infection, hepatotoxicity, lymphomas
Hypertension, tremor, hirsutism, leukopenia
Gingival hyperplasia, gynecomastia
Anaphylaxis, fetal harm

FIRST-GENERATION H1 ANTAGONISTS FIRST-GENERATION H1 ANTAGONISTS
Ch 69 Antihistamines
Antihistamines Antihistamines
Prototype: Diphenhydramine (Benadryl) Prototype: Diphenhydramine (Benadryl)
Mechanism of Action
Blocks H1 receptors
Other First-Generation Antihistamines
Blocks some muscarinic receptors Brompheniramine
Reduces actions of histamine Chlorpheniramine (Chlor-Trimeton)
Reduces flushing, itching, and secretion of mucus Dexchlorpheniramine
Fold here
Clemastine (Tavist)
Uses Promethazine (Phenergan)
Seasonal allergic rhinitis, urticaria, severe allergy, motion sickness, insomnia Hydroxyzine (Vistaril)
Cold symptoms, sleep aid, mild transfusion reactions, allergic reactions
Adverse Effects
Sedation, confusion, fatigue
Paradoxical excitation can occur
Gastrointestinal disturbances
Anticholinergic effects (BUDCAT)

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SECOND-GENERATION (NONSEDATING) H1 SECOND-GENERATION (NONSEDATING) H1
Ch 69 Antihistamines
ANTAGONISTS ANTAGONISTS
Prototype: Loratadine (Claritin) Prototype: Loratadine (Claritin)
Antihistamine Antihistamine
Mechanism of Action
Blocks H1 receptors
Other Second-Generation Nonsedating H1
Reduces actions of histamine Antagonists
Reduces flushing, itching, secretion of mucus Desloratadine (Clarinex)
Fold here
Does not cross brain-blood barrier to cause sedation Fexofenadine (Allegra)

Cetirizine (Zyrtec)
Uses Levocetirizine (Xyzal)
Allergic rhinitis, urticaria, and mild transfusion reactions Azelastine (Astelin) nasal spray
Adverse Effects
Reduce dose if hepatic or renal impairment occurs
Cetirizine (Zyrtec) may cause mild sedation in some patients

CYCLOOXYGENASE INHIBITORS CYCLOOXYGENASE INHIBITORS
Ch 70 Cyclooxygenase Inhibitors: NSAIDs and Acetaminophen

Nonsteroidal Anti-inflammatory Drug (NSAID) Nonsteroidal Anti-inflammatory Drug (NSAID)
Prototype: Aspirin Prototype: Aspirin
Mechanism of Action
Irreversible inhibition of cyclooxygenase (COX-1 and COX-2)
Suppresses platelet aggregation
Decreases prostaglandin synthesis
Reduces inflammation, pain, and fever
Uses
Suppression of inflammation
Fold here
Analgesia
Reduction of fever in adults
Dysmenorrhea
Suppression of platelet aggregation to protect against MI and stroke
Prevention of colorectal cancer
Possible protection against Alzheimer’s disease
Adverse Effects
Gastric distress (heartburn and nausea)
GI bleeding, gastric ulceration and perforation
Not used in children because of the risk of Reye’s syndrome
Fetal harm (prolongs labor, premature closure of the patent ductus)
Salicylism (tinnitus, sweating, headache, dizziness)
Hypersensitivity in patients with allergies
Renal impairment
Bleeding Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
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CYCLOOXYGENASE INHIBITORS CYCLOOXYGENASE INHIBITORS

First Generation—Nonaspirin NSAIDs First Generation—Nonaspirin NSAIDs
Prototype: Ibuprofen (Advil, Motrin)
Prototype: Ibuprofen (Advil, Motrin)
Other NSAIDs
Mechanism of Action Fenoprofen (Nalfon)
Reversible inhibition of COX-1 and COX-2 Flurbiprofen (Ansaid)
Inhibits prostaglandin synthesis Ketoprofen
Naproxen (Aleve, Anaprox, Naprelan, Naprosyn)
Has anti-inflammatory, analgesic, and antipyretic actions Oxaprozin (Daypro)
Diclofenac (Voltaren, Cataflam)—risk of liver failure
Fold here
Uses Voltaren Gel and Flector Patch

Fever, pain, arthritis, dysmenorrhea Diclofenac Plus Misoprostol (Arthrotec)
Diflunisal (Dolobid)
Closure of the ductus arteriosus in preterm infants Etodolac
Indomethacin (Indocin)
Adverse Effects Ketorolac (Toradol), available IM or IV
Bleeding, gastric ulceration, renal impairment Mefenamic acid (Ponstel)
Meclofenamate
Cross-hypersensitivity with aspirin Meloxicam (Mobic)
May precipitate Reye’s syndrome Nabumetone
Fetal harm Piroxicam (Feldene)
Risk of MI and stroke Sulindac (Clinoril)
Tolmetin (Tolectin)

CYCLOOXYGENASE INHIBITOR CYCLOOXYGENASE INHIBITOR

Second-Generation NSAID (COX-2 Inhibitor) Second-Generation NSAID (COX-2 Inhibitor)
Prototype: Celecoxib (Celebrex) Prototype: Celecoxib (Celebrex)
Mechanism of Action
Selective inhibition of COX-2
Decreases prostaglandin synthesis at the site of injury
Reduces pain and inflammation
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
No inhibition of platelets
Increased risk of MI and stroke Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
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ACETAMINOPHEN (TYLENOL) ACETAMINOPHEN (TYLENOL)

Analgesic and Antipyretic Analgesic and Antipyretic
Mechanism of Action
Reduces prostaglandin synthesis in the CNS
Has no anti-inflammatory properties
Uses
Pain and fever
Preferred in children
Fold here
No GI injury, no effect on platelets or kidneys

Adverse Effects
Toxic metabolite builds up in ETOH abusers
Hepatic necrosis can occur
Maximum dose is 4 grams/day
Acetylcysteine (Mucomyst) given for overdose
Inhibits metabolism of warfarin (risk of bleeding)

GLUCOCORTICOIDS GLUCOCORTICOIDS
Ch 71 Glucocorticoids in Nonendocrine Diseases

Mechanism of Action Short Acting
Suppress immune responses and inflammation Cortisone
Inhibit prostaglandins, leukotrienes, and histamine Hydrocortisone
Suppress phagocytes and lymphocytes
Intermediate Acting
Uses Prednisone
Rheumatoid arthritis, SLE, inflammatory bowel disease Prednisolone
Bursitis, osteoarthritis, anaphylaxis, asthma Methylprednisone
Fold here
Skin disorders, neoplasms, suppression of allograft rejection Triamcinolone
Prevention of respiratory distress syndrome (RDS) in preterm infants
Replacement therapy for patients with Addison’s disease Long Acting
Betamethasone
Adverse Effects Dexamethasone
Adrenal insufficiency resulting from suppression of HPA axis
Osteoporosis, infection, glucose intolerance (increases blood sugar)
Myopathy, sodium and water retention, potassium loss
Growth retardation, mood changes
Cataracts, glaucoma
Peptic ulcer disease, iatrogenic Cushing’s syndrome
Fetal harm
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DISEASE-MODIFYING ANTIRHEUMATIC DRUGS DISEASE-MODIFYING ANTIRHEUMATIC DRUGS
Ch 72 Drug Therapy of Rheumatoid Arthritis

(DMARDs I) (DMARDs I)
Prototype: Methotrexate (Rheumatrex, Trexall) Prototype: Methotrexate (Rheumatrex, Trexall)
Mechanism of Action Other DMARDs I
Blocks conversion of folic acid to its active form Sulfasalazine (Azulfidine)
Reduces joint destruction, retards disease progression Leflunomide (Arava)
Takes 3 to 5 months to see effect Hydroxychloroquine (Plaquenil)
Uses DMARDs II
Fold here
Rheumatoid arthritis, non-Hodgkin’s lymphoma Etanercept (Enbrel)

Lymphocytic leukemia, psoriasis, and Crohn’s disease Infliximab (Remicade)
Adalimumab (Humira)
Adverse Effects Rituximab (Rituxan)
Abatacept (Orencia)
Bone marrow suppression, hepatic fibrosis
GI ulceration, pneumonitis, and fetal harm DMARDs III
Penicillamine (Cuprimine)
Azathioprine (Imuran)
Cyclosporine
Anakinra (Kineret)
Protein A column (Prosorba)
DRUGS FOR HYPERURICEMIA DRUGS FOR HYPERURICEMIA
Ch 73 Drug Therapy of Gout

Prototype: Allopurinol (Zyloprim) Prototype: Allopurinol (Zyloprim)
Mechanism of Action
Inhibits uric acid formation
Other Drugs for Hyperuricemia
Probenecid
Uses Sulfinpyrazone (Anturane)
Chronic tophaceous gout
Hyperuricemia secondary to chemotherapy
Drugs for Acute Gouty Arthritis
Not useful for acute gouty attacks NSAIDs
Fold here
Glucocorticoids
Adverse Effects Colchicine (GI toxicities)
Hypersensitivity syndrome
Nausea, vomiting, abdominal discomfort
Drowsiness, headache, metallic taste
Cataracts with prolonged use (#3 years)

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BISPHOSPHONATES BISPHOSPHONATES
Ch 74 Drugs Affecting Calcium Levels and Bone Mineralization

Prototype: Alendronate (Fosamax) Prototype: Alendronate (Fosamax)
Mechanism of Action
Suppresses resorption of bone
Other Bisphosphonates
Reduces both the number and activity of osteoclasts Risedronate (Actonel)
Ibandronate (Boniva)
Uses Tiludronate (Skelid)
Postmenopausal osteoporosis Etidronate (Didronel)
Osteoporosis in men Zoledronate (Reclast, Zometa)
Fold here
Glucocorticoid-induced osteoporosis Other Drugs Used to Treat Osteoporosis

Paget’s disease of the bone
Selective Estrogen Receptor Modulators (SERMs)
Adverse Effects Raloxifene (Evista)
Esophagitis
Musculoskeletal pain, ocular problems Parathyroid Hormone
Osteonecrosis of the jaw Teriparatide (Forteo)
Atrial fibrillation

ANTI-INFLAMMATORY DRUGS FOR ASTHMA ANTI-INFLAMMATORY DRUGS FOR ASTHMA
Ch 75 Drugs for Asthma

INHALED CORTICOSTEROIDS (ICSs) INHALED CORTICOSTEROIDS (ICSs)
Prototype: Fluticasone Propionate (Flovent) Prototype: Fluticasone Propionate (Flovent)
Mechanism of Action
Suppresses the inflammation of asthma
Other Inhaled Corticosteroids
Decreases leukotrienes, histamine, and prostaglandins Beclomethasone dipropionate (QVAR)
Decreases eosinophils and leukocytes Budesonide (Pulmicort Turbohaler, Pulmicort Respules)
Reduces edema of the airway and mucus production Flunisolide (AeroBid)
Reduces bronchial hyperactivity Mometasone furoate (Asmanex Twisthaler)
Fold here
Increases number of beta2 receptors Triamcinolone acetonide (Azmacort)
Increases responsiveness to beta2 agonists
Combination ICSs and Long-Acting Beta2 Agonists
Uses
Fluticasone and salmeterol (Advair)
Control of asthma
Budesonide and formoterol (Symbicort)
Administered on a fixed schedule
Takes 2-8 days to see an effect, maximum benefit in 4-6 weeks
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, glaucoma, and osteoporosis Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
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LEUKOTRIENE MODIFIERS LEUKOTRIENE MODIFIERS
Prototype: Montelukast (Singulair) Prototype: Montelukast (Singulair)
Mechanism of Action
Blocks leukotriene receptors
Other Leukotriene Modifiers
Reduces inflammation, bronchoconstriction, and edema Zileuton (Zyflo)—associated with rare liver injury
Decreases secretion of mucus Zafirlukast (Accolate)—associated with rare liver injury
Reduces eosinophils and other inflammatory cells
Reduces dosage of inhaled corticosteroids
Fold here
Uses
Control of asthma (not used as first-line therapy)
Prevention of exercise-induced bronchospasm
Allergic rhinitis
Not used for rescue
Adverse Effects
GI upset
Delayed effect
Possible rare neuropsychiatric effects (mood changes, suicidal thoughts)

Prototype: Cromolyn (Intal) Prototype: Cromolyn (Intal)
Mechanism of Action
Suppresses inflammation, prevents release of histamine
Stabilizes mast cell membrane
Not a bronchodilator
Uses
Control of asthma
Fold here
Must be given on a fixed schedule (not used for rescue)
Prevents exercise-induced bronchospasm
Allergic rhinitis (intranasal cromolyn)
Adverse Effects
Safest of all antiasthma medications
Rarely, can cause cough or bronchospasm

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BRONCHODILATORS BRONCHODILATORS

BETA2-ADRENERGIC AGONISTS BETA2-ADRENERGIC AGONISTS
(Inhaled Short-Acting Agents) (Inhaled Short-Acting Agents)
Prototype: Albuterol (Proventil, Ventolin, Accuneb) Prototype: Albuterol (Proventil, Ventolin, Accuneb)
Mechanism of Action
Activation of beta2-adrenergic receptors in the lung
Other Beta2-Adrenergic Agonist
Promotes bronchodilation Levalbuterol (Xopenex, Xopenex HFA)
Rapid onset of action for rescue breathing
Oral Beta2-Adrenergic Agonists
Fold here
Suppresses histamine release in the lung

Increases ciliary motility Albuterol (generic) tablets or syrup
Albuterol (VoSpire ER)
Uses Terbutaline (Brethine)
Rapid relief of asthma symptoms (Inhaled beta2 agents are preferred)
Adverse Effects
Tachycardia, angina, and tremor


BETA2-ADRENERGIC AGONISTS BETA2-ADRENERGIC AGONISTS
(Inhaled Long-Acting Agents) (Inhaled Long-Acting Agents)
Prototype: Salmeterol (Serevent) Prototype: Salmeterol (Serevent)
Mechanism of Action
Activates beta2-adrenergic receptors in the lung
Other Long-Acting Inhaled Beta2-Adrenergic Agonists
Promotes bronchodilation Formoterol (Foradil)
Suppresses histamine release in the lung Arformoterol (Brovana)
Fold here
Increases ciliary motility
Uses
Asthma
Should not be used alone
Should be used in conjunction with an ICS
Adverse Effects
Effect is delayed by 20 to 30 minutes
Not to be used for rescue breathing
Tachycardia, angina, tremor, and leg cramps
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METHYLXANTHINES METHYLXANTHINES
Prototype: Theophylline Prototype: Theophylline
Mechanism of Action
Produces bronchodilation by relaxing bronchi
Other Methylxanthines
Aminophylline
Uses
Asthma
(Beta2 agonists and inhaled corticosteroids preferred)
Fold here
Adverse Effects
Narrow therapeutic range (5-15 mcg/mL)
Dysrhythmias, ventricular fibrillation
Convulsions, cardiorespiratory collapse, and death
Many drug-drug reactions

INTRANASAL GLUCOCORTICOIDS (ICSs) INTRANASAL GLUCOCORTICOIDS (ICSs)
Ch 76 Drugs for Allergic Rhinitis, Cough, and Colds

Prototype: Fluticasone (Flonase) Prototype: Fluticasone (Flonase)
Mechanism of Action
Anti-inflammatory actions suppress symptoms of allergic rhinitis
Other Intranasal Glucocorticoids
Prevent or suppress congestion, rhinorrhea, sneezing, nasal itching Beclomethasone (Beconase AQ)
Budesonide (Rhinocort Aqua)
Uses Flunisolide (Nasarel)
Seasonal and perennial rhinitis Mometasone (Nasonex)
Triamcinolone (Nasacort AQ)
Fold here
Adverse Effects
Other Drugs Used for Allergic Rhinitis
Drying of the nasal mucosa, burning or itching
Sore throat, epistaxis (nose bleed), and headache Oral and nasal antihistamines
Intranasal cromolyn sodium (NasalCrom)
Topical sympathomimetics (Oxymetazoline-Afrin)
Oral sympathomimetics (phenylephrine, pseudoephedrine)
Ipratropium bromide (Atrovent) nasal spray
Montelukast (Singulair)

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ANTITUSSIVES ANTITUSSIVES
Ch 76 Drugs for Allergic Rhinitis, Cough, and Colds

Prototype: Dextromethorphan Prototype: Dextromethorphan
Nonopioid Antitussive Nonopioid Antitussive
Mechanism of Action
Acts in the CNS to suppress cough
Other Nonopioid Antitussives
Elevates the cough threshold Diphenhydramine (Benadryl)
Benzonatate (Tessalon)
Uses
Opioid Antitussives
Fold here
Acute cough
Codeine
Adverse Effects Hydrocodone
Mild inebriation and mind-body dissociation when abused
Can increase analgesic response to morphine

HISTAMINE2-RECEPTOR ANTAGONIST HISTAMINE2-RECEPTOR ANTAGONIST
Ch 77 Drugs for Peptic Ulcer Disease

Prototype: Cimetidine (Tagamet) Prototype: Cimetidine (Tagamet)
Mechanism of Action
Blocks H2 receptors on parietal cells of the stomach
Other Histamine2-Receptor Antagonists
Reduces volume of gastric juice and hydrogen ion content Ranitidine (Zantac)
Famotidine (Pepcid)
Uses Nizatidine (Axid)
Gastric and duodenal ulcers
Gastroesophageal reflux disease (GERD)
Fold here
Treatment of Zollinger-Ellison syndrome
Aspiration pneumonitis
Heartburn, acid indigestion, and sour stomach
Adverse Effects
Significant side effects are uncommon
Antiandrogenic effects
Confusion, hallucinations, CNS depression or excitation
Pneumonia

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PROTON PUMP INHIBITORS (PPIs) PROTON PUMP INHIBITORS (PPIs)
Ch 77 Drugs for Peptic Ulcer Disease

Prototype: Omeprazole (Prilosec) Prototype: Omeprazole (Prilosec)
Mechanism of Action
Inhibits the enzyme that generates acid production
Other PPIs
Lansoprazole (Prevacid)
Uses Rabeprazole (Aciphex)
Duodenal and gastric ulcers, erosive esophagitis Pantoprazole (Protonix)
GERD, dyspepsia Esomeprazole (Nexium)
Zollinger-Ellison syndrome Other Antiulcer Drugs
Fold here
Adverse Effects Sucralfate (Carafate)

Headache, diarrhea, nausea, and vomiting Misoprostol (Cytotec)
Gastric cancer, and hip fractures Antacids
Combination Drugs for Helicobacter pylori–associated ulcers
Helidac
Pylera
Prevpac

ANTIEMETIC DRUGS ANTIEMETIC DRUGS
Ch 79 Other Gastrointestinal Drugs

Serotonin-Receptor Antagonists Serotonin-Receptor Antagonists
Prototype: Ondansetron (Zofran) Prototype: Ondansetron (Zofran)
Mechanism of Action
Suppresses emesis by blocking 5-HT3 receptors in the
Other Serotonin-Receptor Antagonists
chemoreceptor trigger zone (CTZ) Granisetron (Kytril)
Dolasetron (Anzemet)
Uses Palonosetron (Aloxi)
Fold here
Reduces nausea and vomiting caused by
chemotherapy, radiation therapy, and anesthesia (postoperatively)
Other Agents Used for Nausea
Glucocorticoids
Adverse Effects Aprepitant (Emend)
Headache, diarrhea, and dizziness Benzodiazepines

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ANTIEMETIC DRUGS ANTIEMETIC DRUGS

Dopamine Antagonists Dopamine Antagonists
Prototype: Prochlorperazine (Compazine) Prototype: Prochlorperazine (Compazine)
Mechanism of Action
Suppresses emesis by blocking dopamine2 receptors in the CTZ
Other Dopamine Antagonists
Phenothiazines
Uses Chlorpromazine (Thorazine)
Nausea and vomiting Perphenazine (Trilafon)
Fold here
Used after surgery, cancer chemotherapy, or other conditions Promethazine (Phenergan)
Adverse Effects Butyrophenones

Extrapyramidal reactions, anticholinergic effects Haloperidol (Haldol)
Hypotension and sedation Droperidol (Inapsine)
Metoclopramide (Reglan)
Cannabinoids
Dronabinol (Marinol)
Nabilone (Cesamet)

PROKINETIC AGENTS PROKINETIC AGENTS

Prototype: Metoclopramide (Reglan) Prototype: Metoclopramide (Reglan)
Mechanism of Action
Suppresses emesis by blocking receptors for dopamine and serotonin in the
chemoreceptor trigger (CTZ)
Increases upper GI motility by enhancing the actions of acetylcholine
Uses
Suppresses postoperative nausea and vomiting
Fold here
Suppresses emesis associated with chemotherapy, radiation therapy, toxins
and opioids
Relieves diabetic gastroparesis
Suppresses gastroesophageal reflux disease (GERD)
Adverse Effects
Sedation and diarrhea
Extrapyramidal reactions, especially in children

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HYDROXYZINE (VISTARIL, ATARAX) HYDROXYZINE (VISTARIL, ATARAX)

Antiemetic Drug Antiemetic Drug
Anticholinergic-Antihistamine Anticholinergic-Antihistamine
Mechanism of Action
Blocks histaminergic and cholinergic receptors
Uses
Nausea
Fold here
Adverse Effects
Sedation, blurry vision, urinary retention, dry mouth

PENICILLINS (PCNs) PENICILLINS (PCNs)
Ch 83 Drugs That Weaken the Bacterial Cell Wall I

Narrow-Spectrum Penicillin (Penicillinase Sensitive) Narrow-Spectrum Penicillin (Penicillinase Sensitive)
Beta-Lactam Antibiotic Beta-Lactam Antibiotic
Prototype: Benzylpenicillin (Penicillin G) Prototype: Benzylpenicillin (Penicillin G)
Mechanism of Action
Disruption of the bacterial cell wall
Parenteral PCN G (three salts)
(1) Potassium PCN G (IM or IV)
Fold here
Uses (2) Procaine PCN G (never used IV)
Parenteral antibiotic treats gram-positive and gram-negative (3) Benzathine PCN G (never used IV)
Streptococcus and Neisseria organisms, anaerobes, and others Prescribed in units (1 unit = 0.6 mg)
Drug of choice for syphilis Oral PCN
Adverse Effects Penicillin V (Veetids)
Allergic reaction, pain at site of injection
Neurotoxicities
Do not mix PCN with aminoglycosides in IV solutions

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ANTISTAPHYLOCCAL PENICILLINS ANTISTAPHYLOCCAL PENICILLINS

Penicillinase-Resistant Penicillins Penicillinase-Resistant Penicillins
(PCNs that cannot be inactivated by bacterial beta-lactamases) (PCNs that cannot be inactivated by bacterial beta-lactamases)
Prototype: Nafcillin (Unipen) Prototype: Nafcillin (Unipen)

Mechanism of Action
Disruption of the bacterial cell wall Other Antistaphyloccal Penicillins
Oxacillin
Uses Dicloxacillin
Fold here
Treats infections caused by penicillinase-producing strains of Staphylococcus Methicillin (no longer available)
(ie, S. aureus, S. epidermidis)
Adverse Effects
Allergic reaction, GI effects
Thrombophlebitis, hypokalemia

AMINOPENICILLINS AMINOPENICILLINS

Broad-Spectrum Antibiotics Broad-Spectrum Antibiotics
Prototype: Amoxicillin Prototype: Amoxicillin
Mechanism of Action
Other Aminopenicillins
Ampicillin
Uses (Amoxicillin is preferred for oral therapy)
Same antimicrobial spectrum as PCN
Fold here
plus increased activity against gram-negative bacilli
Treats infections caused by Haemophilus influenzae, Escherichia coli,
and Salmonella and Shigella organisms
Ineffective against Staphylococcus aureus
Adverse Effects
Diarrhea

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ANTIPSEUDOMONIAL PENICILLINS ANTIPSEUDOMONIAL PENICILLINS

Extended-Spectrum Penicillins Extended-Spectrum Penicillins
Prototypes: Ticarcillin, Piperacillin Prototypes: Ticarcillin, Piperacillin
Mechanism of Action
Antipseudomonal Penicillins with
Beta-Lactamase Inhibitors
Uses Ticarcillin with clavulanic acid (Timentin)
Antimicrobial spectra same as for aminopenicillins Piperacillin with tazobactam (Zosyn)
Fold here
plus Pseudomonas aeruginosa, Bacteroides fragilis,

and Enterobacter, Proteus, and Klebsiella spp.
Used with aminoglycosides (not in the same IV)
Can be destroyed by bacterial penicillinases
Adverse Effects
Sodium overload
Interference with platelet function, leading to increased bleeding time

FIRST-GENERATION CEPHALOSPORINS FIRST-GENERATION CEPHALOSPORINS
Ch 84 Drugs That Weaken the Bacterial Cell Wall II

Beta-Lactam Antibiotics Beta-Lactam Antibiotics
Prototype: Cephalexin (Keflex) Prototype: Cephalexin (Keflex)
Mechanism of Action
Weakens the bacterial cell wall
Other First-Generation Cephalosporins
Cefadroxil (Duricef)
Uses Cefazolin (IV)
Gram-positive infections
Fold here
Surgical prophylaxis
Adverse Effects
Allergic reaction
Pain at injection site
Thrombophlebitis
Rare antibiotic-associated pseudomembranous colitis (AAPMC)

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SECOND-GENERATION CEPHALOSPORINS SECOND-GENERATION CEPHALOSPORINS

Prototype: Cefprozil (Cefzil) Prototype: Cefprozil (Cefzil)
Mechanism of Action
Other Second-Generation Cephalosporins
Cefaclor (Ceclor)
Uses Cefotetan (Cefotan)
Enhanced activity against gram-negative bacteria Cefoxitin (Mefoxin)
Fold here
Upper respiratory tract infections Cefuroxime (Ceftin)

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

THIRD-GENERATION CEPHALOSPORINS THIRD-GENERATION CEPHALOSPORINS

Prototype: Ceftriaxone (Rocephin) Prototype: Ceftriaxone (Rocephin)
Mechanism of Action
Other Third-Generation Antibiotics
Oral
Uses Cefdinir (Omnicef)
Active against gram-negative organisms Cefditoren (Spectracef)
Fold here
Able to penetrate cerebrospinal fluid (CSF) Cefixime (Suprax)
Cefpodoxime (Vantin)
Treats meningitis caused by gram-negative and gram-positive bacteria Ceftibuten (Cedax)
Effective for Neisseria gonorrhoeae infection
IM, IV
Adverse Effects
Cefoperazone (Cefobid)
Allergic reaction Cefotaxime (Claforan)
Thrombophlebitis Ceftazidime (Fortaz) [for Pseudomonas aeruginosa]
Rare antibiotic-associated pseudomembranous colitis (AAPMC) Ceftizoxime (Cefizox)
Fatal precipitate forms with calcium
(Do not mix with Ringer’s lactate) Fourth-Generation Cephalosporin
Cefepime (Maxipime)
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CARBAPENEMS CARBAPENEMS

Broad-Spectrum Beta-Lactam Antibiotics Broad-Spectrum Beta-Lactam Antibiotics
Prototype: Imipenem (Primaxin) Prototype: Imipenem (Primaxin)
Mechanism of Action
Other Carbapenems
Meropenem (Merrem IV)
Uses Ertapenem (Invanz)
Active against gram-positive cocci, Doripenem (Doribax)
Fold here
gram-negative cocci, gram-negative bacilli, and anaerobic bacteria

Adverse Effects
GI effects
Hypersensitivity reactions
Suprainfections
Seizures (rare)

VANCOMYCIN (VANCOCIN) VANCOMYCIN (VANCOCIN)

Antibiotic Antibiotic
Mechanism of Action
Inhibits bacterial cell wall synthesis
Uses
Active against gram-positive bacteria
Effective for serious infections, such as methicillin-resistant Staphylococcus aureus
(MRSA)
Fold here
Second choice to treat antibiotic-associated pseudomembranous colitis
Oral form used in patients who do not respond to metronidazole to delay resistance
Used for patients allergic to penicillin
Adverse Effects
Ototoxicity
Rapid infusion can lead to red man syndrome (ie, flushing,
tachycardia, and hypotension)
Thrombophlebitis
Immune-mediated thrombocytopenia
NOTE: Infuse over 60 minutes or longer

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TETRACYCLINES TETRACYCLINES

Broad-Spectrum Antibiotics Broad-Spectrum Antibiotics
Prototype: Doxycycline (Vibramycin)
Mechanism of Action Prototype: Doxycycline (Vibramycin)
Suppresses bacterial growth by inhibiting protein synthesis
Binds to 30S ribosomal subunit to prevent the addition of amino acids
Bacteriostatic Other Tetracyclines
Uses Tetracycline (Sumycin)
Rocky Mountain spotted fever, typhus fever, Q fever Minocycline (Minocin)
Infections caused by Chlamydia trachomatis
Brucellosis, cholera Demeclocycline (Declomycin)
Fold here
Pneumonia caused by Mycoplasma pneumoniae

Lyme disease, anthrax
Gastric infections with Helicobacter pylori (peptic ulcer disease [PUD])
Periodontal disease and acne
Community-acquired methicillin-resistant S. aureus (CA-MRSA)
Adverse Effects
GI irritation, suprainfection (AAPMC)
Overgrowth with fungi (Candida albicans)
Discoloration of teeth (avoid in children "8 years old)
Do not give to pregnant women
Hepatotoxicity, exacerbation of renal impairment
Photosensitivity, vestibular toxicity
Chelating agents interfere with absorption
Do not administer with:
milk products, calcium, iron, magnesium, and laxatives Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
MACROLIDES MACROLIDES
Ch 85 Bacteriostatic Inhibitors of Protein Synthesis

Broad-Spectrum Antibiotic Broad-Spectrum Antibiotic
Prototype: Erythromycin Prototype: Erythromycin
Mechanism of Action
Inhibits bacterial cell wall synthesis
Other Macrolides
Binds to the 50S ribosomal subunit to block addition of amino acids Clarithromycin (Biaxin)
Azithromycin (Zithromax)
Uses Dirithromycin (Dynabac)
Fold here
Active against most gram-positive and some gram-negative organisms Troleandomycin (Tao)
Treats atypicals such as:
Pneumonia caused by Legionella pneumophila and Mycoplasma pneumoniae
Bordetella pertussis, Corynebacterium diphtheria
Can be used as an alternative to PCN in allergic individuals
Treats chlamydial infections (urethritis, cervicitis)
Adverse Effects
GI effects, liver injury
Inhibitor of cytochrome P450
Increases levels of theophylline, carbamazepine, and some statins
QT prolongation and sudden cardiac death Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
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CLINDAMYCIN (CLEOCIN) CLINDAMYCIN (CLEOCIN)

Antibiotic Antibiotic
Mechanism of Action
Inhibits bacterial protein synthesis
Uses
Used as an alternative to penicillin for serious gram-positive anaerobic
infections
Bacteroides fragilis, Fusobacterium sp., Clostridium perfringens
Fold here
Adverse Effects
Antibiotic-associated pseudomembranous colitis (AAPMC)
Diarrhea

LINEZOLID (ZYVOX) LINEZOLID (ZYVOX)

Oxazolidinones Antibiotic Oxazolidinones Antibiotic
Mechanism of Action
Bacteriostatic inhibitor of protein synthesis
Binds to the 23S portion of the 50S ribosomal subunit
Uses
Active against aerobic and gram-positive bacteria
Enterococcus faecium (vancomycin sensitive and vancomycin resistant)
Fold here
Staphylococcus aureus (methicillin-sensitive and methicillin-resistant strains)
Staphylococcus epidermidis (methicillin-resistant strains)
Streptococcus pneumoniae (PCN sensitive and PCN resistant)
Adverse Effects
GI effects
Myelosuppression (reversible)
Neuropathy
HTN (blocks MAO)

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AMINOGLYCOSIDES AMINOGLYCOSIDES
Ch 86 Aminoglycosides: Bactericidal Inhibitors of Protein Synthesis

Narrow-Spectrum Antibiotics Narrow-Spectrum Antibiotics
Prototype: Gentamicin Prototype: Gentamicin
Mechanism of Action
Disrupts bacterial protein synthesis
Other Aminoglycosides
Binds to the 30S ribosomal subunit Tobramycin
Amikacin (Amikin)
Uses
Fold here
Effective against aerobic gram-negative bacilli

Serratia marcescens, Proteus mirabilis, Pseudomonas aeruginosa
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

SULFONAMIDES AND TRIMETHROPRIM SULFONAMIDES AND TRIMETHROPRIM
Ch 87 Sulfonamides and Trimethoprim

Prototype: Trimethoprim/Sulfamethoxazole Prototype: Trimethoprim/Sulfamethoxazole
(Bactrim, Septra) (Bactrim, Septra)
Mechanism of Action
Combination antibiotic that inhibits bacterial synthesis of folic acid
Uses
Urinary tract infections
Pneumocystis pneumonia (PCP) caused by Pneumocystis jiroveci
Fold here
Adverse Effects
GI effects
Hypersensitivity reactions (Stevens-Johnson syndrome)
Not for use in patients with sulfa allergies
Hematologic effects: Agranulocytosis,
leukopenia, thrombocytopenia, aplastic anemia
Hemolytic anemia in patients with G6PD deficiency
Kernicterus (do not use in infants "2 months or pregnant women near term)
Crystalluria, leading to renal damage (increase fluids)
CNS effects, hyperkalemia, photosensitivity
Increases the effects of sulfonylurea, leading to hypoglycemia Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
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FLUOROQUINOLONES FLUOROQUINOLONES
Ch 90 Miscellaneous Antibacterial Drugs

Prototype: Ciprofloxacin (Cipro) Prototype: Ciprofloxacin (Cipro)
Mechanism of Action
Inhibits bacterial DNA and cell division
Other Fluoroquinolones
Respiratory fluoroquinolones:
Uses Moxifloxacin (Avelox)* and Levofloxacin (Levaquin)
Infections of the urinary, respiratory, and GI tracts, bones, Gemifloxacin (Factive)*
joints, skin, and soft tissues *Prolongs
Anthrax QT interval
Fold here
Adverse Effects
Achilles tendon rupture and tendinitis (black box warning)
GI upset
CNS effects (dizziness, headache, and restlessness)
Do not take with milk products or iron
Elevates levels of warfarin
Not recommended for children under age 18
Avoid in pregnancy

METRONIDAZOLE (FLAGYL) METRONIDAZOLE (FLAGYL)
Ch 90 Miscellaneous Antibacterial Drugs

Antibacterial Drug Antibacterial Drug
Mechanism of Action
Causes cell death by damaging bacterial DNA
Uses
Protozoal infections
Infections caused by obligate anaerobic bacteria (Bacteroides fragilis)
Infections of the CNS, abdominal organs, bones, joints, skin, and soft tissue
Fold here
Infections of the genitourinary tract (Trichomonas vaginalis)
Drug of choice for antibiotic-associated colitis caused by
Clostridium difficile
Eradicates Helicobacter pylori
Used as prophylaxis in colorectal or abdominal surgery
Adverse Effects
Nausea, headache, dry mouth, metallic taste
Vertigo, numbness in the extremities
Dark discoloration of urine
Disulfiram-like effect (vomiting) when used with alcohol
Increases warfarin levels Copyright © 2010 by Saunders, an imprint of Elsevier Inc.
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ANTIFUNGAL AGENTS ANTIFUNGAL AGENTS
Ch 91 Antifungal Agents
Prototype: Itraconazole (Sporanox) Prototype: Itraconazole (Sporanox)
Mechanism of Action
Causes bacterial cell wall to leak
Other Azole Antifungals
Fluconazole (Diflucan)
Uses Voriconazole (Vfend)
Ketoconazole (Nizoral)
Systemic and superficial mycoses (fungi) Posaconazole (Noxafil)
Miconazole (Monistat)
Adverse Effects Clotrimazole
Fold here
GI effects, headache, abdominal pain, and edema

Cardiac suppression Other Antifungal Drugs
Liver injury Amphotericin B (causes nephrotoxicity)
Inhibits hepatic drug-metabolizing enzymes Caspofungin (Cancidas)
Drug reactions with digoxin, warfarin, sulfonylureas, statins, Micafungin (Mycamine)
proton pump inhibitors (PPIs) Anidulafungin (Eraxis)
Flucytosine (Ancibon)
Nystatin (Mycostatin)
Terbinafine (Lamisil)
Butenafine (Lotrimin)
Ciclopirox (Loprox, Penlac Nail Lacquer)

ANTIFUNGAL AGENT ANTIFUNGAL AGENT
Ch 91 Antifungal Agents
Griseofulvin Griseofulvin
Mechanism of Action
Inhibits fungal mitosis
Uses
Superficial mycoses (fungi)
Dermatophytic infections of the skin, hair, and nails
Not active against Candida species or systemic mycoses
Fold here
May take 3 to 8 weeks to have an effect
Adverse Effects
May diminish effects of warfarin

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ANTIVIRAL DRUGS ANTIVIRAL DRUGS
Ch 92 Antiviral Agents I
Prototype: Acyclovir (Zovirax) Prototype: Acyclovir (Zovirax)
Mechanism of Action
Suppresses synthesis of viral DNA
Valacyclovir (Valtrex)
Uses Famciclovir (Famvir)
Herpes simplex genitalis
Mucocutaneous herpes simplex infections
Topical Agents
Varicella-zoster infections Penciclovir (Denavir)
Fold here
Docosanol (Abbreva)
Adverse Effects
IV administration can lead to phlebitis and nephrotoxicity
Ocular Agents
Infuse slowly over 1 hour and maintain hydration Trifluridine (Viroptic)
Oral therapy may lead to nausea, vomiting, diarrhea Vidarabine ointment (Vira-A)
Headache and vertigo

DRUGS FOR HEPATITIS DRUGS FOR HEPATITIS
Prototype: Interferon Alpha Prototype: Interferon Alpha
Mechanism of Action
Decreases viral replication
Uses
Hepatitis B and hepatitis C
Adverse Effects
Fold here
Flulike syndrome
Neuropsychiatric effects—depression and suicidal ideation
Fatigue, thyroid dysfunction, heart damage
Bone marrow suppression

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DRUGS FOR HEPATITIS DRUGS FOR HEPATITIS
Prototype: Ribavirin (Rebetol, Copegus) Prototype: Ribavirin (Rebetol, Copegus)
Mechanism of Action
Unclear
Uses
Used with interferon for treatment of hepatitis C
Adverse Effects
Fold here
Hemolytic anemia
Fetal harm (FDA Pregnancy Risk Category X)
Use a second reliable form of birth control during treatment
and for 6 months after treatment

NUCLEOSIDE/NUCLEOTIDE REVERSE TRANSCRIPTASE NUCLEOSIDE/NUCLEOTIDE REVERSE TRANSCRIPTASE
Ch 93 Antiviral Agents II
INHIBITORS (NRTIs) INHIBITORS (NRTIs)
Antiretroviral Drugs Antiretroviral Drugs
Prototype: Zidovudine (Retrovir) Prototype: Zidovudine (Retrovir)
Mechanism of Action
Suppress the synthesis of viral DNA by blocking transcriptase
Other NRTIs and Combinations
Penetrates the CNS better than most antiretrovirals Didanosine (Videx)
Stavudine (Zerit)
Fold here
Uses Lamivudine (Epivir)
HIV infection Abacavir (Ziagen)
Tenofovir disoproxil fumarate (Viread)
Adverse Effects Emtricitabine (Emtriva)
Anemia and neutropenia from bone marrow suppression Zalcitabine (Hivid)
Lactic acidosis with hepatomegaly and hepatic steatosis Abacavir/zidovudine/lamivudine (Trizivir)
Gastrointestinal effects Abacavir/lamivudine (Epzicom)
CNS reactions (headache, insomnia, confusion, anxiety, and seizures) Emtricitabine/tenovir (Truvada)
Myopathy Lamivudine/zidovudine (Combivir)
Emtricitabine/tenofovir/efavirenz (Atripla)

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NON-NUCLEOSIDE REVERSE TRANSCRIPTASE NON-NUCLEOSIDE REVERSE TRANSCRIPTASE
INHIBITORS (NNRTIs) INHIBITORS (NNRTIs)
Prototype: Efavirenz (Sustiva) Prototype: Efavirenz (Sustiva)
Mechanism of Action
Binds directly to HIV reverse transcriptase
Other NNRTIs
Inhibits reverse transcriptase Nevirapine (Viramune)
Delavirdine (Rescriptor)
Fold here
Uses Etravirine (Intelence)

HIV infection
Adverse Effects
CNS symptoms
Rash, Stevens-Johnson syndrome
Fetal harm
Liver damage
Many drug-drug reactions

PROTEASE INHIBITORS PROTEASE INHIBITORS
Prototype: Ritonavir (Norvir) Prototype: Ritonavir (Norvir)
Mechanism of Action
Inhibits the enzyme protease, which HIV requires to mature
Other Protease Inhibitors
Lopinavir/ritonavir (Kaletra)
Uses Indinavir (Crixivan)
HIV infection Saquinavir (Invirase)
Fold here
Nelfinavir (Viracept)
Adverse Effects Amprenavir (Agnerease)
Fosamprenavir (Lexiva)
Hyperglycemia/diabetes, fat maldistribution, hyperlipidemia
Atazanavir (Reyataz)
Increased bleeding in hemophiliac patients
Tipranavir (Aptivus)
Reduced bone mineral density
Darunavir/ritonavir (Prezista)
Elevation of serum transaminases
Can increase or decrease levels of other drugs
Many drug-drug interactions

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INTEGRASE INHIBITORS INTEGRASE INHIBITORS
Prototype: Raltegravir (Isentress) Prototype: Raltegravir (Isentress)
Mechanism of Action
Inhibits integrase to stop HIV replication
Other Drugs for HIV
Uses HIV Fusion Inhibitor

HIV infection Enfuvirtide (Fuzeon)
Fold here
Adverse Effects Chemokine Receptor CCR5 Antagonist

Diarrhea, nausea, fatigue, headache, and itching Maraviroc (Selzentry)
Possible myopathy and rhabdomyolysis

Commonly Used Dietary Supplements Commonly Used Dietary Supplements
Ch 107 Dietary Supplements

Dietary Dietary
Supplement Uses Potential Problems Supplement Uses Potential Problems
Ginkgo biloba Improves age-related memory May suppress coagulation Black cohosh Menopausal symptoms Liver toxicity
Glucosamine Osteoarthritis Increased risk of bleeding Comes mixed with St. John’s
Green tea Improves mental clarity, Increased heart rate, hepatotoxicity wort; many drug-drug reactions
weight loss, cancer prevention Reduces effects of warfarin Coenzyme Q-10 May reduce myalgias May antagonize the effects of
Kava Anxiety Hepatotoxicity, sedation associated with statins warfarin
Ma huang Stimulant Stroke, MI, and death Cranberry juice Prevents bacteria from GI upset and formation of uric
Probiotics Irritable bowel syndrome, Flatulence adhering to urinary tract acid kidney stones
Fold here
antibiotic-associated diarrhea Echinacea Stimulates immune system Allergic reactions
Saw palmetto Benign prostatic hypertrophy Suppresses platelet Feverfew Migraine prophylaxis Suppresses platelet
aggregation-risk of bleeding aggregation-risk of bleeding
Fetal harm in women Flaxseed Dyslipidemia and constipation Suppresses platelet
Soy Prevention of cancer Increased risk of oxalate aggregation-risk of bleeding
Menopausal symptoms Kidney stones Garlic Dyslipidemia and hypertension Suppresses platelet
St. John’s wort Mild to moderate depression Photosensitivity aggregation-risk of bleeding
Accelerates metabolism of Ginger root Vertigo, nausea, and vomiting Suppresses platelet
many drugs Anti-inflammatory effects aggregation-risk of bleeding
Serotonin syndrome High doses can cause
Valerian root Sedative, promotes sleep Drowsiness spontaneous abortion

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Common Drug Endings-cont’d Common Drug Endings

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

Ch 9 Drug Therapy During Pregnancy and Breast-Feeding

Antithyroid drugs (propylthiouracil, methimazole) Category C: Greater risk than B

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

CH 13 Physiology of he Peripheral Nervous System

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MUSCARINIC AGONISTS MUSCARINIC AGONISTS

Ch 14 Muscarinic Agonists and Antagonists

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

Ch 14 Muscarinic Agonists and Antagonists

Sources of Muscarinic Poisoning

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

MUSCARINIC ANTAGONISTS MUSCARINIC ANTAGONISTS

Ch 14 Muscarinic Agonists and Antagonists

Ch 14 Muscarinic Agonists and Antagonists

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

ANTICHOLINERGIC DRUGS FOR OVERACTIVE ANTICHOLINERGIC DRUGS FOR OVERACTIVE

Ch 14 Muscarinic Agonists and Antagonists

Overactive bladder (urge incontinence) Trospium (Sanctura, Sanctura XR)

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

Ch 15 Cholinesterase Inhibitors and Their Use in Myasthenia Gravis

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

Ch 16 Drugs That Block Nicotinic Cholinergic Transmission

Short operative procedures

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

ADRENERGIC AGONISTS ADRENERGIC AGONISTS

Mechanism of Action Other Sympathomimetics Used for Nasal Congestion

Treatment of nasal congestion

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

BETA-ADRENERGIC ANTAGONISTS BETA-ADRENERGIC ANTAGONISTS

Labetalol (Trandate) blocks beta1, beta2, and alpha1 receptors

BETA-ADRENERGIC ANTAGONISTS BETA-ADRENERGIC ANTAGONISTS

Uses Nebivolol (Bystolic) blocks beta receptors

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

Ch 19 Indirect-Acting Antiadrenergic Agents

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

DOPAMINERGICS FOR PARKINSON’S DISEASE DOPAMINERGICS FOR PARKINSON’S DISEASE

Ch 21 Drugs for Parkinson’s Disease

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

Other Drugs for Alzheimer’s Disease

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

ANTIEPILEPTIC DRUGS (AEDs) ANTIEPILEPTIC DRUGS (AEDs)

Ch 24 Drugs for Epilepsy

All AEDs may increase suicidal thoughts and behaviors

Ch 24 Drugs for Epilepsy

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

MUSCLE RELAXANTS MUSCLE RELAXANTS

Ch 25 Drugs for Muscle Spasm and Spasticity

CNS depression Cyclobenzaprine ER (Amrix)

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

GENERAL ANESTHESTICS GENERAL ANESTHETICS

Respiratory and cardiac depression Thiopental sodium (Pentothal)

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

Ch 28 Opioid (Narcotic) Analgesics and Antagonists

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

AGONIST-ANTAGONIST OPIOIDS AGONIST-ANTAGONIST OPIOIDS

Ch 28 Opioid (Narcotic) Analgesics and Antagonists

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

Ch 28 Opioid (Narcotic) Analgesics and Antagonists

Copyright © 2010 by Saunders, an imprint of Elsevier Inc.

NONOPIOID CENTRALLY ACTING ANALGESICS NONOPIOID CENTRALLY ACTING ANALGESICS