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ReceptorSubtype
Alpha1
Alpha2
Beta1
Beta2
Dopamine
Location
EyeArterioles (skin, viscera, mucous
membranes)VeinsSex organs, maleBladder neck and prostatic capsulePresynaptic nerve terminals
Heart
KidneyArterioles (heart, lung, and
skeletal mucle)BronchiUterusLiverSkeletal muscleKidney
Response to Receptor Activation
Mydriasis—wide eyed with fearConstriction
ConstrictionEjaculationContractionInhibition of transmitter release—decreases
sympathetic nervous system (SNS) out-flow to the blood vessels and heart
Increased rate, force of contraction, and AVconduction velocity
Renin release—RASDilation
DilationRelaxationGlycogenolysisEnhanced contraction, glycogenolysisDilation of kidney vasculature
Drug Receptor TypesFunctions of Peripheral Adrenergic Receptor Subtypes
Receptor Subtype
Nicotinicn
Nicotinicm
Muscarinic
Location
All autonomic nervous systemganglia and the adrenal medulla
Neuromuscular junctionAll parasympathetic target organs:
EyeHeartLung
BladderGI tract
Sweat glandsSex organsBlood vessels
Response to Receptor Activation
Stimulation of parasympathetic andsympathetic postganglionic nerves andrelease of epinephrine from the adrenalmedulla
Contraction of skeletal muscle
MiosisDecreased rateConstriction of bronchiPromotion of secretionsVoidingSalivationIncreases gastric secretions, intestinal
tone, and motilityDefecationGeneralized sweatingErectionVasodilation
Functions of Peripheral Cholinergic Receptor Subtypes
Drug EndingsDrug Endings
-zosin-olol, -lol-zepam, -zolam-pril-artan-dipine-statin-ase, -plase-parin-sone-dronate
Drug Classification
Alpha-adrenergic blockerBeta-adrenergic blockerBenzodiazepine (BZD)Angiotensin-converting enzyme (ACE) inhibitorAngiotensin-receptor blocker (ARB)Calcium channel blockerLipid-lowering drugThrombolyticAnticoagulantCorticosteroidBisphosphonate for osteoporosis
Drug Example
prazosinmetoprololdiazepam, alprazolamlisinoprilcandesartanamlodipineatorvastatinalteplaseenoxaparinprednisonealendronate
Drug Endings—cont’dDrug Endings
-terol-tidine-prazole-cillin-cef, -ceph-cycline-floxacin-thromycin-micin, -mycin-azole
Drug Classification
BronchodilatorHistamine2 blocker–acid reducerProtein pump inhibitor–acid reducerPenicillin antibioticCephalosporin antibioticTetracycline antibioticFluoroquinolone antibioticMacrolide antibioticAminoglycoside antibioticAntifungal
Drug Example
albuterolcimetidineomeprazoleamoxicillincefazolintetracyclinelevofloxacinazithromycingentamycinitraconazole
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BETHANECHOL (URECHOLINE)Muscarinic Agonist
Activates muscarinic receptorsCauses contraction of the detrusor muscle of the bladder
UsesPostoperative urinary retention
Adverse EffectsHypotension
Bradycardia, dysrhythmiasBronchoconstriction
GI effects
BETHANECHOL (URECHOLINE)
Muscarinic Agonist
ATROPINEMuscarinic Antagonist (Anticholinergic)
Blocks muscarinic receptorsIncreases heart rate
Decreases salivary, bronchial, sweat, and acid-secreting cell secretionsRelaxes bronchial smooth muscles
Decreases bladder tone and GI motilityDilates pupils (mydriasis)
UsesPreanesthesia to prevent bradycardia, treatment of bradycardia
Dilation of pupil for ocular examination or surgeryIntestinal hypertonicity and hypermotilityAntidote for muscarinic-agonist poisoning
Adverse EffectsBlurry vision, urinary retention, dry mouth, constipation, tachycardia
Increases intraocular pressure
ATROPINE
Muscarinic Antagonist (Anticholinergic)
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NEOSTIGMINE (PROSTIGMINE)Reversible Cholinesterase Inhibitor
Prevents the degradation of acetylcholine (ACh)Enhances the effect of ACh to stimulate skeletal muscle
UsesMyasthenia gravis
Reversal of neuromuscular blockade in postoperative patients
Adverse EffectsExcessive glandular secretions, increased GI motilityUrinary urgency, bradycardia, sweating, and miosis
Cholinergic crisis—treat with atropine
NEOSTIGMINE (PROSTIGMINE)
Reversible Cholinesterase Inhibitor
SUCCINYLCHOLINEDepolarizing Neuromuscular Blocker
Causes paralysis of muscle by preventing repolarization
UsesMuscle relaxation during endotracheal intubation
Used for short operative procedures
Adverse EffectsProlonged paralysis in genetically determined individuals
Malignant hyperthermia—treat with dantroleneMuscle pain, hyperkalemia
SUCCINYLCHOLINE
Depolarizing Neuromuscular Blocker
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PHENYLEPHRINEAdrenergic Agonist
Activates alpha1 receptorsConstricts blood vessels of the skin, viscera, and mucous membranes
UsesTreatment of nasal congestionDelay of anesthetic absorption
Dilation of the pupil for ocular exam
Adverse EffectsHypertension
Necrosis
PHENYLEPHRINE
Adrenergic Agonist
EPINEPHRINEAdrenergic Agonist (Catecholamine)
Activates all four adrenergic receptors—alpha1, alpha2, beta1, and beta2Pupil dilation, arterial and venous vasoconstriction
Increases heart rate and force of contractionBronchial dilation, glycogenolysis, enhanced muscle contraction
UsesCardiac arrest, heart failure, and anaphylactic shock
AV heart block and asthmaDelays absorption of local anesthetic and controls superficial bleeding
Reduces nasal congestionDilates pupil for eye procedures
Adverse EffectsHypertension, tachycardia, and dysrhythmias
Angina, necrosis following extravasationHyperglycemia in diabetic patients
EPINEPHRINE
Adrenergic Agonist (Catecholamine)
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PROPRANOLOL (INDERAL)Adrenergic Antagonist
Noncardioselective Beta Blocker
Blocks beta1 and beta2 receptorsReduces heart rate, decreases force of ventricular contraction
Decreases conduction through AV node, decreases cardiac outputSuppresses renin, bronchoconstriction
UsesAngina, hypertension, cardiac dysrhythmias
Myocardial infarction, heart failure, hyperthyroidism, glaucoma
Adverse EffectsBradycardia, reduced cardiac output, AV heart block
Rebound cardiac excitation, bronchoconstrictionInhibition of glycogenolysis, CNS effects
Not used in patients with asthma or diabetes
PROPRANOLOL (INDERAL)
Adrenergic AntagonistNoncardioselective Beta Blocker
METOPROLOL (LOPRESSOR, TOPROL XL)Adrenergic Antagonist
Cardioselective Beta Blocker
Blocks cardiac beta1 receptorsReduces heart rate, decreases force of ventricular contraction
Decreases conduction through AV node, decreases cardiac outputSuppresses renin
Does not block beta2 receptors (no bronchoconstriction)Not likely to inhibit glycogenolysis
Preferred for patients with asthma or diabetes
UsesHypertension, angina pectoris, heart failure
Adverse EffectsBradycardia, reduction of cardiac output, AV heart blockRebound cardiac excitation following abrupt withdrawal
METOPROLOL (LOPRESSOR, TOPROL XL)
Adrenergic AntagonistCardioselective Beta Blocker
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PRAZOSIN (MINIPRESS)Adrenergic Antagonist
Alpha blocker
Blocks alpha1 receptorsDilates arteries and veins
Relaxes smooth muscle in the bladder neck and prostatic capsule
UsesHypertension
Benign prostatic hypertrophy
Adverse EffectsOrthostatic hypotension, reflex tachycardia
Inhibition of ejaculationNasal congestion
Use with sildenafil (Viagra), other drugs for erectile dysfunction, can lead to hypotension
PRAZOSIN (MINIPRESS)
Adrenergic AntagonistAlpha Blocker
CLONIDINE (CATAPRES)Centrally Acting Alpha2 Agonist
Antihypertensive Drug
Activates alpha2 receptors in the CNSReduces sympathetic flow to the heart and blood vessels
Reduces stimulation of adrenergic receptors in the peripheryNet effect of cardiac suppression and vasodilation is decreased
blood pressure
UsesHypertension
Adverse EffectsHypotension
Bradycardia, decrease in cardiac outputDrowsiness, dry mouth
Rebound hypertension in response to abrupt withdrawalFetal harm
CLONIDINE (CATAPRES)
Centrally Acting Alpha2 AgonistAntihypertensive Drug
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LEVODOPA/CARBIDOPA (SINEMET)Dopaminergic Agent
Levodopa increases synthesis of dopamine in the striatumCarbidopa enhances the effect of levodopa
UsesReduces symptoms of Parkinson’s disease
Adverse EffectsEffects take several months to develop
Loss of effect occurs over timeNausea, vomiting, dyskinesias
Postural hypotension, psychosisDark sweat and urine, may activate melanoma
LEVODOPA/CARBIDOPA (SINEMET)
Dopaminergic Agent
DONEPEZIL (ARICEPT)Cholinesterase Inhibitor
Prevents the breakdown of AChIncreases ACh at cholinergic synapses
May slow progression of Alzheimer’s disease (AD)Some improvement of cognitive function
UsesAlzheimer’s disease (AD)
Adverse EffectsCholinergic effects
Nausea, vomiting, dyspepsia, diarrheaBradycardia, bronchoconstriction
DONEPEZIL (ARICEPT)
Cholinesterase Inhibitor
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PHENYTOIN (DILANTIN)Antiepileptic Drug (AED)
Inhibits entry of sodium into neuronsSuppresses action potential of neurons
UsesEpilepsy
Adverse EffectsNystagmus, sedation, ataxia, diplopia
Cognitive impairment, gingival hyperplasia, hirsutismRash, fetal harm, bleeding tendencies in newborns
Narrow therapeutic range (10 to 20 mcg/mL)Can decrease the effect of other drugs such as:
Oral contraceptives, warfarin, and glucocorticoidsInject slowly, use normal saline flush
Withdraw over a period of 6 to 8 weeks to avoid seizures
PHENYTOIN (DILANTIN)
Antiepileptic Drug (AED)
VALPROIC ACID (DEPAKOTE)Antiepileptic Drug (AED)
Blocks sodium channels to suppress neuronsSuppresses calcium influx
Increases inhibitory influence of gamma-aminobutyric acid (GABA)
UsesEpilepsy, bipolar disorder, migraine headaches
Adverse EffectsNausea, vomiting, indigestion
Hepatotoxicity, pancreatitis, fetal harmWeight gain, rash, hair loss, tremor
Blood dyscrasias
VALPROIC ACID (DEPAKOTE)
Antiepileptic Drug (AED)
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MORPHINEOpioid Analgesic
Activates mu receptorsProduces analgesia, euphoria, sedation
UsesRelief of pain
Adverse EffectsRespiratory depression, constipation
Orthostatic hypotension, urinary retention, miosisBiliary colic, euphoria, sedation, cough suppression
Tolerance and physical dependenceReversed with naloxone (Narcan)
MORPHINE
Opioid Analgesic
NALOXONE (NARCAN)Opioid Antagonist
Reverses the effects of opioids
UsesOpioid overdose
Reversal of excessive respiratory depression
Adverse EffectsMinimal
NALOXONE (NARCAN)
Opioid Antagonist
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SUMATRIPTAN (IMITREX)Serotonin1B/1D-Receptor Agonist (Triptan)
Binds to 5-HT1B/1D receptors to cause vasoconstrictionReduces release of inflammatory peptides
Diminishes perivascular inflammation
UsesMigraine headache
Adverse EffectsChest pressure, coronary vasospasm
Fetal harm
SUMATRIPTAN (IMITREX)
Serotonin1B/1D-Receptor Agonist (Triptan)
CONVENTIONAL ANTIPSYCHOTICS(NEUROLEPTICS)
Relieve positive symptoms of schizophreniaBlock receptors for dopamine, acetylcholine (ACh), histamine, and
norepinephrine (NE)
UsesSchizophrenia, bipolar disorder, Tourette’s syndrome, and dementia
Adverse EffectsExtrapyramidal symptoms (EPS) (acute dystonia, parkinsonism, akathisia,
tardive dyskinesia)Neuroleptic malignant syndrome
Anticholinergic effects, orthostatic hypotensionSedation, neuroendocrine effects, seizures
Sexual dysfunction, increased risk of sunburnAgranulocytosis, dysrhythmias
CONVENTIONAL ANTIPSYCHOTICS(NEUROLEPTICS)
Chlorpromazine (Thorazine)Thioridazine (Mellaril)Haloperidol (Haldol)
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ATYPICAL ANTIPSYCHOTICSRelieve positive and negative signs and symptoms of schizophreniaBlock receptors for serotonin, dopamine, ACh, histamine, and NE
Clinically superior to conventional antipsychotics
UsesSchizophrenia
Adverse EffectsSedation, orthostatic hypotension, weight gain, dry mouthBlurry vision, urinary retention, constipation, tachycardia
Galactorrhea, gynecomastia, amenorrhea, diabetesAgranulocytosis, seizures
Low risk of extrapyramidal effects
ATYPICAL ANTIPSYCHOTICSClozapine (Clozaril)
Risperidone (Risperdal)Olanzapine (Zyprexa)Quetiapine (Seroquel)Ziprasidone (Geodon)Aripiprazole (Abilify)
SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs)
Antidepressants
Inhibit serotonin reuptake (more serotonin is available at the synapse)
UsesMajor depression, OCD
Panic disorder, PTSD, PMDD
Adverse EffectsSexual dysfunction, nausea, headache, insomnia
Weight gain, serotonin syndromeWithdrawal syndrome
SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs)
Fluoxetine (Prozac)Paroxetine (Paxil)Sertraline (Zoloft)
Citalopram (Celexa)Escitalopram (Lexapro)
Antidepressants
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TRICYCLIC ANTIDEPRESSANTS (TCAs)Antidepressants
Inhibit reuptake of NE and serotonin (more serotonin and NE available atthe synapse)
UsesDepression, bipolar disorder, insomnia, and neuropathic pain
Adverse EffectsOrthostatic hypotension, sedation
Anticholinergic effectsCardiotoxicity, seizures, hypomania
Many drug interactionsSSRIs preferred for treatment of depression
TRICYCLIC ANTIDEPRESSANTS (TCAs)Amitriptyline (Elavil)
Clomipramine (Anafranil)Desipramine (Norpramin)
Doxepin (Sinequan)
Antidepressants
MONOAMINE OXIDASE INHIBITORS (MAOIs)Antidepressants
Increase NE and serotonin by blocking enzyme that inactivates them
UsesDepression
Adverse EffectsCNS stimulation, orthostatic hypotension
Hypertensive crisis from buildup of dietary tyramineMany drug interactions
SSRIs preferred for treatment of depression
MONOAMINE OXIDASE INHIBITORS (MAOIs)
Antidepressants
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LITHIUMMood-Stabilizing Drug
Mechanism unclear, may alter ions and neurotransmitters
UsesStabilizes mood in patients with bipolar disorder
Reduces euphoria, hyperactivity, and other symptomsPreferred for patients with classic (euphoric) mania
Adverse EffectsAccumulates to toxic levels in the presence of a low sodium level
Lithium levels must be kept below 1.5 mEq/LBlood levels drawn 12 hours after evening dose
Signs of toxicity include fine hand tremor, GI upset, thirst, polyuria, andmuscle weakness
Chronic use can lead to renal toxicity and hypothyroidismPregnancy Risk Category D
Drug interactions occur with diuretics, NSAIDs, and anticholinergics
LITHIUM
Mood-Stabilizing Drug
VALPROIC ACID (DEPAKOTE)Mood-Stabilizing Anticonvulsant
Suppresses mania and stabilizes mood
UsesMood stabilizer for patients with bipolar disorder
Adverse EffectsGI disturbances, weight gain
Rare thrombocytopenia, pancreatitis, liver failureTarget trough level is 50 to 125 mg/mL
VALPROIC ACID (DEPAKOTE)
Mood-Stabilizing Anticonvulsant
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LAMOTRIGINE (LAMICTAL)Newer Mood-Stabilizing Anticonvulsant
Shows some efficacy in treating bipolar disorder
UsesBipolar disorder
Adverse EffectsHeadache, dizziness, double vision
Life-threatening rashes include Stevens-Johnson syndrome and epidermal necrolysis
LAMOTRIGINE (LAMICTAL)
Newer Mood-Stabilizing Anticonvulsant
BENZODIAZEPINES (BZDs)Sedative Hypnotic Drugs
Depress central nervous system functionReduce anxiety, promote sleep
Potentiate the actions of GABA (an inhibitory neurotransmitter)
UsesAnxiety, insomnia, seizure disorder, induction of anesthesiaMuscle spasm, panic disorder, and withdrawal from alcohol
Adverse EffectsCNS depression, anterograde amnesia, paradoxic effects
Weak respiratory depression if given orallyIV administration can cause severe respiratory depression
Abuse and addiction, teratogenicDo not mix with other CNS depressants or alcohol
Reversal agent is flumazenil (Romazicon)
BENZODIAZEPINES (BZDs)Alprazolam (Xanax)Diazepam (Valium)
Flurazepam (Dalmane)Lorazepam (Ativan)Midazolam (Versed)
Temazepam (Restoril)
Sedative-Hypnotic Drugs
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ZOLPIDEM (AMBIEN)Sedative-Hypnotics
BZD-like Drugs
Potentiate the actions of GABA (an inhibitory neurotransmitter)
UsesShort-term management of insomnia
Adverse EffectsDaytime drowsiness, dizziness
Do not use with alcohol or other CNS depressants
ZOLPIDEM (AMBIEN)ZALEPLON (SONATA)
Sedative-HypnoticsBZD-like Drugs
BARBITURATESCNS Depressants
Potentiate the actions of GABA (an inhibitory neurotransmitter)
UsesInsomnia
Suppression of seizures, induction of general anesthesia
Adverse EffectsRespiratory depression, decreased blood pressure and heart rateInduction of hepatic drug-metabolizing enzymes (increases the
metabolism of other drugs)May lead to tolerance and dependenceFrequently used as vehicles for suicide
Teratogenic
BARBITURATESThiopental (Pentothal)Secobarbital (Seconal)
Phenobarbital
CNS Depressants
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METHYLPHENIDATE(RITALIN, METADATE, CONCERTA)
CNS Stimulant for ADHD
Promotes norepinephrine (NE) and dopamine (DA) releaseInhibits NE and DA reuptake
UsesAttention deficit/hyperactivity disorder (ADHD)
Narcolepsy
Adverse EffectsInsomnia, reduced appetite, palpitations, hypertension, angina,
dysrhythmias, psychosisAbrupt discontinuation can lead to withdrawal reactions
Potential for abuse (Schedule II)Sudden death
METHYLPHENIDATE(RITALIN, METADATE, CONCERTA)
CNS Stimulant for ADHD
ATOMOXETINE (STRATTERA)Nonstimulant Drug for ADHD
Selective inhibitor of NE reuptakeCauses NE to accumulate at synapses
UsesADHD in children and adults
Adverse EffectsGI reactions, reduced appetite, dizziness, and somnolence
Urinary retention, mood swings, insomnia, sexual dysfunction
ATOMOXETINE (STRATTERA)
Nonstimulant Drug for ADHD
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ADDERALLCNS Stimulant Used for ADHD
Combination Amphetamine
UsesADHD
Adverse EffectsInsomnia, growth suppression
Headache, abdominal pain, lethargyAbuse potential (Schedule II)
Sudden deathDrug holidays recommended
ADDERALL
CNS Stimulant Used for ADHDCombination Amphetamine
DISULFIRAM (ANTABUSE)Aversion Therapy for Alcoholism
Disrupts alcohol metabolism by blocking enzymeAldehyde accumulates and produces unpleasant effects
UsesAlcohol abuse
Adverse EffectsNausea, vomiting, flushing, palpitations, headache
Sweating, blurry vision, hypotension, chest pain, shockwill occur with 7 mL of alcohol ingestion
DISULFIRAM (ANTABUSE)
Aversion Therapy for Alcoholism
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FUROSEMIDE (LASIX)Loop Diuretic
Blocks reabsorption of sodium and chloride in the descending limb of theloop of Henle to promote urination
Produces profound diuresis
UsesRapid mobilization of fluid
Pulmonary edema resulting from heart failure or renal or liver diseaseEspecially useful in patients with renal insufficiency
Adverse EffectsHypokalemia, hyponatremia, hypochloremia, dehydration, hypotension,
and ototoxicityMay cause dysrhythmias when used with digoxin (decreases potassium)
FUROSEMIDE (LASIX)
Loop Diuretic
HYDROCHLOROTHIAZIDE (HCTZ)Thiazide Diuretic
Blocks reabsorption of sodium and chloride in the early segment of thedistal convoluting tubule to promote urination
UsesTreatment of hypertension
Mobilization of edema with mild heart failure, hepatic or renal disease
Adverse EffectsHyponatremia, hypochloremia, dehydration
Hypokalemia and hypotension
HYDROCHLOROTHIAZIDE (HCTZ)
Thiazide Diuretic
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SPIRONOLACTONE (ALDACTONE)Potassium-Sparing Diuretic
Blocks the actions of aldosterone in the distal nephronCauses the retention of potassium and increased excretion of sodium
UsesHypertension and edema
Heart failurePrimary hyperaldosteronism
Adverse EffectsEndocrine effects such as:
Gynecomastia, menstrual irregularities, impotence, and hirsutismHyperkalemia
SPIRONOLACTONE (ALDACTONE)
Potassium-Sparing Diuretic
ENALAPRIL (VASOTEC)Angiotensin-Converting Enzyme (ACE) Inhibitor
Inhibits ACE, reducing levels of angiotensin IIDilates arterioles and veins to reduce BP
Reduces blood volume
UsesHypertension, heart failure, MI, diabetic nephropathy
Prevention of MI, stroke, and death
Adverse EffectsHypotension, cough, hyperkalemia
Renal failure in patients with renal artery stenosisFetal injuryAngioedema
ENALAPRIL (VASOTEC)Benazepril (Lotensin)Fosinopril (Monopril)
Lisinopril (Prinivil and Zestril)Moexipril (Univasc)Perindopril (Aceon)Quinapril (Accupril)
Ramipril (Altace)Trandolapril (Mavik)
Angiotensin-Converting Enzyme (ACE) Inhibitors
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LOSARTAN (COZAAR)Angiotensin II-Receptor Blocker (ARB)
Blocks the actions of angiotensin IIDilates arterioles and veins to reduce BP
Reduces blood volume
UsesHypertension, heart failure, MI, and diabetic nephropathy
Prevention of MI, stroke, and death
Adverse EffectsRenal failure in patients with renal artery stenosis
HypotensionAngioedemaFetal injury
Does not cause cough or hyperkalemia
LOSARTAN (COZAAR)Candesartan (Atacand)Eprosartan (Teveten)Olmesartan (Benicar)
Telmisartan (Micardis)Valsartan (Diovan)
Angiotensin II-Receptor Blockers (ARBs)
VERAPAMIL (CALAN)DILTIAZEM (CARDIZEM)
Calcium Channel Blockers (CCBs)Nondihydropyridines
Block calcium channels in the heart and blood vesselsReduce BP by blocking calcium channels in the arterioles
Increase coronary perfusionBlock SA and AV nodes to reduce heart rate and contractility
Decrease force of contraction
UsesAngina, hypertension, cardiac dysrhythmias
Adverse EffectsConstipation, dizziness, facial flushing, edema, hypotension
Bradycardia, AV block, decreased cardiac contractility
VERAPAMIL (CALAN)DILTIAZEM (CARDIZEM)
Calcium Channel Blockers (CCBs)Nondihydropyridines
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AMLODIPINE (NORVASC)Calcium Channel Blocker
Dihydropyridine
Blocks calcium channels in the blood vesselsVasodilation in peripheral arterioles lowers blood pressure
UsesHypertension
Angina
Adverse EffectsPeripheral edema, flushing, dizziness, headache
Does not slow heart rate like nondihydropyridines
AMLODIPINE (NORVASC)
Calcium Channel BlockerDihydropyridine
DIGOXIN (LANOXIN)Cardiac Glycoside
Positive Inotropic AgentDrug for Heart Failure
Increases the force of ventricular contractionInhibits Na�, K�-ATPase to increase Ca�� inside myocytes
Competes with K� for binding to Na�, K�-ATPase↓K → ↑ Na�, K�-ATPase inhibition → digoxin toxicity
Changes electrical activity of the heart and slows heart rate
UsesHeart failure and dysrhythmias
Adverse EffectsAnorexia, 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 minutesGive Digibind for digoxin overdose
DIGOXIN (LANOXIN)
Cardiac GlycosidePositive Inotropic AgentDrug for Heart Failure
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AMIODARONE (CORDARONE)Antidysrhythmic
Class III Potassium Channel Blocker
Delays repolarizationReduces automaticity in the SA node, reduces contractility
Decreases conduction velocity in the AV node, ventricles, and His-Purkinje system
UsesRecurrent ventricular fibrillationUnstable ventricular tachycardia
Adverse EffectsWidening of the QRS complex
Prolongation of the PR and QT intervalsPulmonary toxicities, sinus bradycardia, AV block, hypotension
Corneal microdeposits, optic neuropathyHepatitis, thyroid dysfunction
Toxicities in pregnancyGrapefruit juice increases levels to toxicity
AMIODARONE (CORDARONE)
AntidysrhythmicClass III Potassium Channel Blocker
VERAPAMIL (CALAN)DILTIAZEM (CARDIZEM)
AntidysrhythmicsClass IV Calcium Channel Blockers
Block calcium channels in the heartSlow SA node automaticity, delay AV nodal conduction
Reduce myocardial contractility
UsesAtrial fibrillation or atrial flutter
Supraventricular tachycardia
Adverse EffectsBradycardia, AV block, and heart failure
Hypotension, peripheral edema, and constipationCan elevate digoxin levels
Grapefruit juice increases levels to toxicity
VERAPAMIL (CALAN)DILTIAZEM (CARDIZEM)
AntidysrhythmicsClass IV Calcium Channel Blockers
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PROCAINAMIDE (PRONESTYL)Antidysrhythmic
Class IA Sodium Channel Blocker
Blocks cardiac sodium channelsSlows conduction in the atria, ventricles, and His-Purkinje system
Delays depolarization
UsesAtrial and ventricular dysrhythmias
Adverse EffectsSystemic lupus erythematous–like syndrome
Blood dyscrasiasQRS widening and prolongation
PROCAINAMIDE (PRONESTYL)
AntidysrhythmicClass IA Sodium Channel Blocker
LIDOCAINE (XYLOCAINE)Antidysrhythmic
Class IB Sodium Channel Blocker
Blocks cardiac sodium channelsSlows conduction in the atria, ventricles, and His-Purkinje system
Reduces automaticity in the ventricles and His-Purkinje systemAccelerates repolarization
UsesShort-term therapy for ventricular dysrhythmias
Adverse EffectsNo significant impact on the ECG
Drowsiness, confusion, and paresthesiasToxic doses may produce convulsions and respiratory arrest
LIDOCAINE (XYLOCAINE)
AntidysrhythmicClass IB Sodium Channel Blocker
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PROPRANOLOL (INDERAL)Antidysrhythmic
Class II Beta Blocker
Beta-adrenergic antagonistBlocks both beta1 and beta2 receptors
Decreases automaticity of the SA nodeDecreases velocity of conduction through the AV node
Decreases myocardial contractility
UsesSinus tachycardia, severe recurrent ventricular tachycardia
Paroxysmal atrial tachycardia, hypertension
Adverse EffectsProlongs PR interval on the ECG
Bradycardia, heart failure, AV block, and sinus arrestBronchospasm in patients with asthma
PROPRANOLOL (INDERAL)
AntidysrhythmicClass II Beta Blocker
ATORVASTATIN (LIPITOR)Lipid-Lowering Drug
HMG-CoA Reductase Inhibitor (Statin)
Inhibits the enzyme that synthesizes cholesterolIncreases the number of LDL receptors to remove LDL
Slows progression of CHD, stabilizes plaque
UsesHypercholesterolemia
Primary prevention of CHD
Adverse EffectsHepatotoxicity, increases ALT and AST
Myopathy, increases CK levels, rhabdomyolysis, dark urine, renal failurePregnancy Risk Category X
Headache, rash, GI complaintsCyclosporine, macrolide antibiotics, azole antifungals, and HIV protease
inhibitors raise some statins to toxic levels
ATORVASTATIN (LIPITOR)FLUVASTATIN (LESCOL)
LOVASTATIN (MEVACOR)PRAVASTATIN (PRAVACHOL)
SIMVASTATIN (ZOCOR)ROSUVASTATIN (CRESTOR)
Lipid-Lowering DrugsHMG-CoA Reductase Inhibitors (Statins)
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NICOTINIC ACID (NIACIN)Lipid-Lowering Agent
Reduces LDL and triglyceridesIncreases HDL
UsesDyslipidemia
Adverse EffectsHepatotoxicity
Flushing, itchingGastric upset, nausea, vomiting, diarrhea
May raise blood sugar in patients with diabetesMay increase incidence of gout
NICOTINIC ACID (NIACIN)
Lipid-Lowering Agent
CHOLESTYRAMINE (QUESTRAN)Bile-Acid Sequestrant
Forms insoluble complex with bile acidsIncreases LDL receptors
Safest of all lipid-lowering drugs
UsesHypercholesterolemia
Often used in combination with statin
Adverse EffectsConstipation, bloating, indigestion
Reduces uptake of fat-soluble vitaminsInterferes with absorption of other drugs
CHOLESTYRAMINE (QUESTRAN)COLESEVELAM (WELCHOL)
Bile-Acid Sequestrants
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GEMFIBROZIL (LOPID)Fibric Acid Derivative (Fibrate)
Decreases triglycerides by lowering VLDLRaises HDL levels
UsesHypertriglyceridemia
Adverse EffectsMyopathy, liver injury
Rash, nausea, abdominal pain, diarrheaGallstone formation
Increases warfarin levels, leading to hemorrhage
GEMFIBROZIL (LOPID)FENOFIBRATE (TRICOR)
Fibric Acid Derivatives (Fibrates)
EZETIMIBE (ZETIA)Cholesterol-Lowering Drug
Blocks cholesterol absorption in the small intestine
UsesHypercholesterolemia
Used in combination with statins
Adverse EffectsMay increase risk of liver damage when used with statin
May increase risk of gallstone formation
EZETIMIBE (ZETIA)
Cholesterol-Lowering Drug
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NITROGLYCERINEOrganic Nitrate
Dilates veins, decreases venous return to the heartDecreases preload
Decreases cardiac oxygen demand
UsesAngina, myocardial infarction
Adverse EffectsHeadache, orthostatic hypotension
Reflex tachycardiaUse with sildenafil (Viagra), other drugs for erectile dysfunction may lead
to severe hypotension
NITROGLYCERINE
Organic Nitrate
CLOPIDOGREL (PLAVIX)Adenosine Diphosphate–Receptor Antagonist
ADP Receptor BlockerAntiplatelet Drug
Blocks enzyme so that platelets are unable to aggregate
UsesPrevention of stroke and MI
Adverse EffectsHemorrhage
CLOPIDOGREL (PLAVIX)
Adenosine Diphosphate–Receptor AntagonistADP Receptor Blocker
Antiplatelet Drug
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EPTIFIBATIDE (INTEGRILIN)Glycoprotein llb/llla–Receptor Antagonists
Antiplatelet Drug—”Super Aspirin”
Interferes with the final step in platelet aggregation
UsesAcute coronary syndromeUsed during angioplasty
Adverse EffectsIntercranial hemorrhage, gastrointestinal bleeding
Hematuria, gingival bleedingThrombocytopenia
Anaphylaxis
EPTIFIBATIDE (INTEGRILIN)
Glycoprotein llb/llla–Receptor AntagonistsAntiplatelet Drug—”Super Aspirin”
ALTEPLASE (tPA)Thrombolytic Drug
Converts plasminogen to plasminPlasmin is an enzyme that digests the fibrin matrix of clots
UsesAcute myocardial infarction, pulmonary embolism, and ischemic stroke
Adverse EffectsBleeding
Intracranial hemorrhage
ALTEPLASE (tPA)
Thrombolytic Drug
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HEPARINParenteral Anticoagulant
Suppresses the formation of fibrin in veinsInactivates clotting factors thrombin and Xa
Anticoagulant effect develops quickly
UsesPrevents venous thrombosis
Used for pulmonary embolism, evolving stroke, DVTOpen heart surgery, MI, renal dialysis
MonitoringActivated partial thromboplastin time (aPTT)
Normal aPTT 40 seconds; therapeutic level 60 to 80 seconds
Adverse EffectsBleeding—antidote is protamine sulfate
Heparin-induced thrombocytopenia (HIT)(Decreased platelet count �100,000 leads to thrombosis)
May be used during pregnancy
HEPARIN
Parenteral Anticoagulant
WARFARIN (COUMADIN)Oral Anticoagulant
Suppresses coagulation by antagonizing vitamin KBlocks synthesis of factors VII, IX, X, and prothrombin
Effect takes a few days
UsesLong-term prophylaxis of venous thrombosisUsed in patients with mechanical heart valves
Used in patients with atrial fibrillation
MonitoringProthrombin time (PT)—reported as INR
Goal INR for atrial fibrillation is 2–3Goal INR for mechanical valves is 3–4.5
Adverse EffectsHemorrhage—antidote is vitamin K
Fetal harm
WARFARIN (COUMADIN)
Oral Anticoagulant
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Copyright © 2007 by Saunders, an imprint of Elsevier Inc.
FERROUS SULFATEOral Iron Preparation
UsesIron deficiency anemia (microcytic hypochromic anemia)
Adverse EffectsNausea, heartburn, bloating, constipation, diarrhea
Liquid iron preparation stains teethToxic to children (lethal dose is 2 to 10 grams)
FERROUS SULFATE
Oral Iron Preparation
CYANOCOBALAMIN (VITAMIN B12)Essential for synthesis of DNA
Catalyzes conversion of folic acid to its active form
UsesB12 deficiency, pernicious anemia
Macrocytic normochromic anemia (megaloblastic anemia)
Adverse EffectsHypokalemia
CYANOCOBALAMIN (VITAMIN B12)
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Copyright © 2007 by Saunders, an imprint of Elsevier Inc.
FOLIC ACID (FOLATE)Essential for synthesis of DNA
UsesTreatment of folic acid deficiency (megaloblastic anemia)
Used prophylactically to prevent neural tube defects (NTDs)
Adverse EffectsFolic acid does not correct neurologic consequencesWill correct anemia, but may mask B12 deficiency
Always give folic acid with B12
FOLIC ACID (FOLATE)
OPRELVEKIN (INTERLEUKIN-11)Thrombopoietic Growth Factor
Stimulates production of platelets (thrombocytes)
UsesUsed in patients undergoing chemotherapy to increase platelets
Adverse EffectsRetention of sodium and water by kidney
Peripheral edemaAnemia, dyspnea, tachycardia
OPRELVEKIN (INTERLEUKIN-11)
Thrombopoietic Growth Factor
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EPOETIN ALFA (ERYTHROPOIETIN)Hematopoietic Growth Factor
Stimulates production of red blood cells
UsesAnemia of chronic renal failure
Anemia due to AIDS treatment with AZT (zidovudine)Anemia caused by chemotherapy
Adverse EffectsHypertension
Increase in cardiovascular eventsRed cell aplasia
EPOETIN ALFA (ERYTHROPOIETIN)
Hematopoietic Growth Factor
FILGRASTIM (NEUPOGEN)Granulocyte Colony Stimulating Factor (G-CSF)
Acts on bone marrow to increase production of neutrophils
UsesUsed in patients undergoing chemotherapy
Decreases risk of infection
Adverse EffectsBone pain, leukocytosis
Elevates uric acid levels, LDH, and alkaline phosphataseSplenomegaly
FILGRASTIM (NEUPOGEN)
Granulocyte Colony Stimulating Factor (G-CSF)
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GLIPIZIDE (GLUCOTROL)Oral Hypoglycemic Agent
Sulfonylurea
Stimulates insulin release from the pancreas
UsesType 2 diabetes
Adverse EffectsHypoglycemia
Fetal harm
GLIPIZIDE (GLUCOTROL)GLYBURIDE (MICRONASE)GLIMEPIRIDE (AMARYL)
Oral Hypoglycemic AgentsSulfonylureas
METFORMIN (GLUCOPHAGE)Oral Hypoglycemic Agent
Biguanide
Decreases blood sugar by decreasing production of glucose in the liverEnhances glucose uptake and utilization in muscle
UsesType 2 diabetes
Adverse EffectsDecreased appetite, nausea, diarrhea, and weight loss
Lactic acidosisAvoid in patients with renal or liver disease
Avoid in patients with ETOH abuse, infection, or CHFDiscontinue 48 hours prior to test with contrast media to avoid
lactic acidosis
METFORMIN (GLUCOPHAGE)
Oral Hypoglycemic AgentBiguanide
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ROSIGLITAZONE (AVANDIA)Thiazolidinedione (TZD)
“Glitazone”Insulin Sensitizer
Increases insulin sensitivity
UsesType 2 diabetes
Adverse EffectsFluid retention—caution in patients with CHF
Hepatotoxicity—monitor ALT
ROSIGLITAZONE (AVANDIA)PIOGLITAZONE (ACTOS)
Thiazolidinediones (TZDs)“Glitazones”
Insulin Sensitizers
MIGLITOL (GLYSET)ACARBOSE (PRECOSE)
Alpha-Glucosidase InhibitorsHypoglycemic Agent
Delay absorption of carbohydratesLower postprandial blood glucose levels
UsesType 2 diabetes
Adverse EffectsFlatulence, cramps, abdominal distention, diarrhea
Hypoglycemia, liver dysfunction
MIGLITOL (GLYSET)ACARBOSE (PRECOSE)
Alpha-Glucosidase InhibitorsHypoglycemic Agents
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REPAGLINIDE (PRANDIN)NATEGLINIDE (STARLIX)
MeglitinidesHypoglycemic Agents
Stimulate pancreatic insulin release
UsesType 2 diabetes
Adverse EffectsHypoglycemia
Administer 30 minutes before meal
REPAGLINIDE (PRANDIN)NATEGLINIDE (STARLIX)
MeglitinidesHypoglycemic Agents
GLUCAGONHormone that increases plasma levels of glucose
Opposite effect of insulin
UsesTreats hypoglycemia from insulin overdose
Used only if IV glucose is not available
GLUCAGON
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LEVOTHYROXINE (SYNTHROID, LEVOXYL)Thyroid Replacement Hormone
Synthetic Preparation of T4
Converted to T3 in the bodyThyroid hormone replacement
UsesHypothyroidism
Adverse EffectsThyrotoxicosis if dosage is excessive
Tachycardia, angina, nervousness, insomniaHyperthermia, sweating, and tremor
Increases warfarin levelsTakes about 1 month to reach plateau
LEVOTHYROXINE (SYNTHROID, LEVOXYL)
Thyroid Replacement HormoneSynthetic Preparation of T4
PROPYLTHIOURACIL (PTU)Antithyroid Drug
Inhibits thyroid hormone synthesis
UsesHyperthyroidism, Graves’ disease
Thyrotoxic crisis
Adverse EffectsAgranulocytosis, hypothyroidism, rash
Fetal harm
PROPYLTHIOURACIL (PTU)
Antithyroid Drug
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GLUCOCORTICOIDSSuppress immune responses and inflammation
Inhibit prostaglandins, leukotrienes, and histamineSuppress phagocytes and lymphocytes
UsesRheumatoid arthritis, SLE, inflammatory bowel disease
Bursitis, osteoarthritis, anaphylaxis, asthmaSkin disorders, prevention of respiratory distress syndrome (RDS) in
preterm infantsReplacement therapy for patients with Addison’s disease
Adverse EffectsAdrenal insufficiency resulting from suppression of HPA axis
Glucose intolerance (increases blood sugar), osteoporosis, infectionGrowth retardation, mood changes, cataracts, glaucoma
Peptic ulcer disease, iatrogenic Cushing’s syndrome
GLUCOCORTICOIDS
SILDENAFIL (VIAGRA)Erectile Dysfunction Drug
Enhances the normal erectile response to sexual stimuli by inhibiting PDE-5
UsesErectile dysfunction
Adverse EffectsHypotension, priapism, headache, and flushing
Visual changesUse with nitrates and alpha blockers leads to hypotension
SILDENAFIL (VIAGRA)TADALAFIL (CIALIS)
VARDENAFIL (LEVITRA)
Erectile Dysfunction Drugs
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PRAZOSIN (MINIPRESS)Alpha-Adrenergic Antagonist
Alpha Blocker
Blocks alpha1 receptorsDilates arteries and veins
Relaxes smooth muscle in the bladder neck and prostatic capsule
UsesBenign prostatic hypertrophy
Hypertension
Adverse EffectsOrthostatic hypotension, reflex tachycardia
Inhibition of ejaculationNasal congestion
Use with erectile dysfunction drugs may lead to hypotension
PRAZOSIN (MINIPRESS)
Alpha-Adrenergic AntagonistAlpha Blocker
LIVE VIRUS VACCINESLive virus vaccines are contraindicated in pregnancyGive with caution in immunocompromised patients
LIVE VIRUS VACCINESVaricella (Varivax)
Oral Polio Vaccine (OPV) not used in the United StatesMeasles, Mumps, and Rubella Virus Vaccine (MMR)
Live Influenza Attenuated Vaccine (LIAV)
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CYCLOSPORINE (SANDIMMUNE)Immunosuppressant Drug
Suppresses production of inflammatory cellsDecreases B cells and cytotoxic T cells
UsesOrgan transplant
Adverse EffectsNephrotoxicity, infection, hepatotoxicity, lymphomas
Hypertension, anaphylaxis, fetal harm
CYCLOSPORINE (SANDIMMUNE)
Immunosuppressant Drug
METHOTREXATE (RHEUMATREX, TREXALL)Cytotoxic Drug
ImmunosuppressantDisease-Modifying Antirheumatic Drug (DMARD)
Blocks conversion of folic acid to its active formReduces joint destruction, retards disease progression
Takes 3 to 5 months to see effect
UsesRheumatoid arthritis, non-Hodgkin’s lymphoma
Lymphocytic leukemia, psoriasis
Adverse EffectsBone marrow suppression, hepatic fibrosisGI ulceration, pneumonitis, and fetal harm
METHOTREXATE (RHEUMATREX, TREXALL)
Cytotoxic DrugImmunosuppressant
Disease-Modifying Antirheumatic Drug (DMARD)
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DIPHENHYDRAMINE (BENADRYL)First-Generation H1 Antagonist
Antihistamine
Blocks H1 receptorsBlocks some muscarinic receptors
Reduces actions of histamineDecreases flushing, itching, and secretion of mucus
UsesAllergic rhinitis, urticaria, motion sickness, insomnia
Cold symptoms, mild transfusion reactions, allergic reactions
Adverse EffectsSedation, confusion, nausea, and dry throat
DIPHENHYDRAMINE (BENADRYL)
First-Generation H1 AntagonistAntihistamine
LORATADINE (CLARITIN)Second-Generation Nonsedating H1
Antagonist (Antihistamine)
Blocks H1 receptorsReduces actions of histamine
Decreases flushing, itching, secretion of mucusDoes not cross blood-brain barrier to cause sedation
UsesAllergic rhinitis, urticaria, and mild transfusion reactions
Adverse EffectsDecrease dose if hepatic or renal impairment occurs
Cetirizine (Zyrtec) may cause mild sedation in some patients
LORATADINE (CLARITIN)DESLORATADINE (CLARINEX)FEXOFENADINE (ALLEGRA)
CETIRIZINE (ZYRTEC)
Second-Generation Nonsedating H1Antagonists (Antihistamines)
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ASPIRINAntiplatelet Drug
Cyclooxygenase (COX) InhibitorFirst-Generation NSAID
Suppresses platelet aggregation by inhibiting COX-1 and COX-2Decreases prostaglandin synthesis
Reduces inflammation, pain, and fever
UsesPain, fever, inflammation
Prevention of thrombus in arteriesPrevents MI and stroke
Adverse EffectsBleeding, gastric ulceration, renal impairment
Not used in children because of Reye’s syndromeFetal harm, salicylism
Hypersensitivity in patients with allergies
ASPIRIN
Antiplatelet DrugCyclooxygenase (COX) Inhibitor
First-Generation NSAID
IBUPROFEN (ADVIL, MOTRIN)First-Generation NSAID
Inhibits cyclooxygenase (COX)-1 and COX-2Inhibits prostaglandin synthesis
Has antiinflammatory, analgesic, and antipyretic actions
UsesDysmenorrhea, arthritis, pain, and fever
Adverse EffectsBleeding, gastric ulceration, renal impairment
Cross-hypersensitivity with aspirinMay precipitate Reye’s syndrome, fetal harm
IBUPROFEN (ADVIL, MOTRIN)
First-Generation NSAID
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CELECOXIB (CELEBREX)Second-Generation NSAID
COX-2 Inhibitor
Selective inhibition of COX-2, decreases prostaglandin synthesis (painand inflammation reduced)Spares COX-1 inhibition
Minimal gastric, renal, and platelet effect
UsesOsteoarthritis, rheumatoid arthritis, dysmenorrhea
Acute pain
Adverse EffectsDyspepsia, mild renal impairment
Not used in patients with sulfonamide allergyPremature closure of ductus arteriosus
CELECOXIB (CELEBREX)
Second-Generation NSAIDCOX-2 Inhibitor
ACETAMINOPHEN (TYLENOL)Analgesic
Antipyretic
Decreases prostaglandin synthesis in the CNSDevoid of antiinflammatory properties
UsesPain and fever
Preferred in childrenNo GI injury, no effect on platelets or kidneys
Adverse EffectsToxic metabolite builds up in ETOH abusers
Hepatic necrosis can occurAcetylcysteine (Mucomyst) given for overdose
ACETAMINOPHEN (TYLENOL)
AnalgesicAntipyretic
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FLUTICASONE PROPIONATE (FLOVENT)Inhaled Corticosteroid (ICS)
Suppresses inflammationDecreases leukotrienes, histamine, and prostaglandins
Decreases eosinophils and leukocytesReduces edema of airway and mucous production
Reduces bronchial hyperactivityIncreases number and responsiveness of beta2 receptors
UsesAsthma
Adverse EffectsOropharyngeal candidiasis—rinse mouth after use
Minimal adrenal suppression and bone lossSlows growth but does not reduce adult heightSlight increased risk of cataracts and glaucoma
FLUTICASONE PROPIONATE (FLOVENT)
Inhaled Corticosteroid (ICS)
SALMETEROL (SEREVENT)Long-Acting Inhaled Beta2-Adrenergic Agonist
Activates beta2 receptors in the lungPromotes bronchodilation
Suppresses histamine release in the lungIncreases ciliary motility
UsesAsthma
Adverse EffectsEffect is delayed by 20 to 30 minutes
Not to be used as a rescue inhaler in an emergencyTachycardia, angina, tremor, and leg cramps
SALMETEROL (SEREVENT)
Long-Acting Inhaled Beta2-Adrenergic Agonist
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MONTELUKAST (SINGULAIR)Leukotriene Modifier
Blocks leukotriene receptorsDecreases inflammation, bronchoconstriction, and edema
Decreases mucous secretionDecreases eosinophils and other inflammatory cells
Reduces dosage of inhaled corticosteroid (ICS)
UsesAsthma and allergic rhinitis
Adverse EffectsGI upset
Effect is delayed
MONTELUKAST (SINGULAIR)
Leukotriene Modifier
THEOPHYLLINEMethylxanthineBronchodilator
Produces bronchodilation by relaxing bronchi
UsesAsthma (beta2 agonists and corticosteroids preferred)
Adverse EffectsNarrow therapeutic range (5 to 10 mcg/mL)
Dysrhythmias, ventricular fibrillationConvulsions, cardiorespiratory collapse, and death
THEOPHYLLINE
MethylxanthineBronchodilator
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ALBUTEROL (PROVENTIL, VENTOLIN, ACCUNEB)Beta2-Adrenergic Agonist
Bronchodilator
Stimulates beta2 receptors in the lungBronchodilation
Rapid onset of action for rescue breathing
UsesAsthma
Adverse EffectsHyperglycemia, tachycardia, tremor
ALBUTEROL (PROVENTIL, VENTOLIN, ACCUNEB)
Beta2-Adrenergic AgonistBronchodilator
RANITIDINE (ZANTAC)Histamine2-Receptor Antagonist
Blocks H2 receptors on parietal cells of the stomachReduces volume of gastric juice and hydrogen ion content
UsesGastric and duodenal ulcers
Gastroesophageal reflux disease (GERD), dyspepsiaTreatment of Zollinger-Ellison syndrome
Adverse EffectsSignificant side effects are uncommon
RANITIDINE (ZANTAC)CIMETIDINE (TAGAMET)FAMOTIDINE (PEPCID)
NIZATIDINE (AXID)
Histamine2-Receptor Antagonists
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OMEPRAZOLE (PRILOSEC)Proton Pump Inhibitor (PPI)
Inhibits the enzyme that generates acid production
UsesDuodenal and gastric ulcers, GERD, dyspepsia
Zollinger-Ellison syndrome
Adverse EffectsHeadache, diarrhea, nausea, and vomiting
OMEPRAZOLE (PRILOSEC)LANSOPRAZOLE (PREVACID)
RABEPRAZOLE (ACIPHEX)PANTOPRAZOLE (PROTONIX)ESOMEPRAZOLE (NEXIUM)
Proton Pump Inhibitors (PPIs)
SUCRALFATE (CARAFATE)Antiulcer drug
Creates a protective barrier against acid and pepsinSticky gel adheres to ulcer crater
UsesDuodenal and gastric ulcers
Adverse EffectsMay impede the absorption of some drugsSeparate at least 2 hours from other drugs
SUCRALFATE (CARAFATE)
Antiulcer drug
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METOCLOPRAMIDE (REGLAN)Prokinetic Drug
Reduces emesis by blocking receptors in the chemoreceptor trigger zone (CTZ)
Increases upper GI motility by enhancing the actions of ACh
UsesSuppresses nausea caused by chemotherapySuppresses postoperative emesis and GERD
Adverse EffectsSedation and diarrhea
Extrapyramidal reactions, especially in children
METOCLOPRAMIDE (REGLAN)
Prokinetic Drug
SULFASALAZINE (AZULFIDINE)Aminosalicylate
Reduces inflammation
UsesInflammatory bowel disease
Crohn’s disease and ulcerative colitis
Adverse EffectsNausea, fever, rash, and arthralgias
Agranulocytosis, hemolytic anemia, and macrocytic anemia
SULFASALAZINE (AZULFIDINE)
Aminosalicylate
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ONDANSETRON (ZOFRAN)Antiemetic Drug
Serotonin-Receptor Antagonist
Suppresses emesis by blocking 5-HT3 receptors in the chemoreceptortrigger zone (CTZ)
UsesDecreases nausea and vomiting due to:
Chemotherapy, radiation therapy, and anesthesia (postoperatively)
Adverse EffectsHeadache, nausea, and dizziness
ONDANSETRON (ZOFRAN)
Antiemetic DrugSerotonin-Receptor Antagonist
PROCHLORPERAZINE (COMPAZINE)Antiemetic Drug
Dopamine Antagonist
Suppresses emesis by blocking dopamine2 receptors in the CTZ
UsesNausea and vomiting
Used after surgery, cancer chemotherapy, or other conditions
Adverse EffectsExtrapyramidal reactions, anticholinergic effects
Hypotension and sedation
PROCHLORPERAZINE (COMPAZINE)PROMETHAZINE (PHENERGAN)
Antiemetic DrugsDopamine Antagonists
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HYDROXYZINE (VISTARIL, ATARAX)Antiemetic Drug
Anticholinergic-Antihistamine
Blocks histaminergic and cholinergic receptors
UsesNausea
Adverse EffectsSedation, blurry vision, urinary retention, dry mouth
HYDROXYZINE (VISTARIL, ATARAX)
Antiemetic DrugAnticholinergic-Antihistamine
PENICILLIN G (BENZYLPENICILLIN)Narrow-Spectrum Penicillin
Weakens the bacterial cell wall
UsesTreats Streptococcus, Neisseria, anaerobes, and others
Drug of choice for syphilis
Adverse EffectsAllergic reaction, pain at site of injection
Neurotoxicities
PENICILLIN G (BENZYLPENICILLIN)
Narrow-Spectrum Penicillin
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NAFCILLIN (UNIPEN)Penicillinase-Resistant Penicillin(Antistaphylococcal Penicillin)
Weakens the cell wall
UsesTreats infections caused by Staphylococcus aureus
Adverse EffectsAllergic reaction, GI effects
Thrombophlebitis, hypokalemia
NAFCILLIN (UNIPEN)
Penicillinase-Resistant Penicillin(Antistaphylococcal Penicillin)
AMOXICILLIN (AMOXIL)Broad-Spectrum Penicillin (Aminopenicillin)
Weakens the bacterial cell wall
UsesTreats infections caused by Haemophilus influenzae, Escherichia coli,
Proteus mirabilis, enterococciNeisseria gonorrhoeae
Adverse EffectsDiarrhea
AMOXICILLIN (AMOXIL)
Broad-Spectrum Penicillin (Aminopenicillin)
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Copyright © 2007 by Saunders, an imprint of Elsevier Inc.
CEFAZOLIN (KEFZOL, ANCEF)First-Generation Cephalosporin
Beta-Lactam Antibiotic
Weakens the bacterial cell wall
UsesGram-positive infections
Surgical prophylaxis
Adverse EffectsAllergic reaction
Bleeding tendenciesThrombophlebitis
Antibiotic-associated pseudomembranous colitis (AAPMC)
CEFAZOLIN (KEFZOL, ANCEF)
First-Generation CephalosporinBeta-Lactam Antibiotic
CEFUROXIME (CEFTIN)Second-Generation Cephalosporin
Beta-Lactam Antibiotic
Weakens the bacterial cell wall
UsesUpper respiratory tract infections
Acute otitis media (AOM) and sinusitis
Adverse EffectsAllergic reaction
Bleeding tendenciesThrombophlebitis
Antibiotic-associated pseudomembranous colitis (AAPMC)
CEFUROXIME (CEFTIN)
Second-Generation CephalosporinBeta-Lactam Antibiotic
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CEFTRIAXONE (ROCEPHIN)Third-Generation Cephalosporin
Beta-Lactam Antibiotic
Weakens the bacterial cell wall
UsesActive against gram-negative organisms
Adverse EffectsAllergic reaction
Bleeding tendenciesThrombophlebitis
Antibiotic-associated pseudomembranous colitis (AAPMC)
CEFTRIAXONE (ROCEPHIN)
Third-Generation CephalosporinBeta-Lactam Antibiotic
VANCOMYCIN (VANCOCIN)Antibiotic
Inhibits bacterial cell wall synthesis
UsesActive against gram-positive bacteria
Serious infections, such as methicillin-resistant Staphylococcus aureus (MRSA)
Antibiotic-associated pseudomembranous colitis (AAPMC)Used for patients allergic to penicillin
Adverse EffectsOtotoxicity
Rapid infusion can lead to “red man syndrome” (flushing, tachycardia,and hypotension)
Infuse over 60 minutes or moreThrombophlebitis
VANCOMYCIN (VANCOCIN)
Antibiotic
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TETRACYCLINEBroad-Spectrum Antibiotic
Suppresses bacterial growth by inhibiting protein synthesis
UsesRocky Mountain spotted fever, typhus
Chlamydia trachomatis, Mycoplasma pneumoniaHelicobacter pylori, anthrax, and Lyme diseaseAcne, peptic ulcer disease, periodontal disease
Adverse EffectsGI irritation, suprainfection (AAPMC)
Discoloration of teeth (avoid in children �8 years old)Hepatotoxicity, exacerbation of renal impairment
Photosensitivity, vestibular toxicity
TETRACYCLINEDOXYCYCLINEMINOCYCLINE
Broad-Spectrum Antibiotics
ERYTHROMYCINMacrolide Antibiotic
Broad-Spectrum Antibiotic
Inhibits bacterial cell wall synthesis
UsesActive against most gram-positive and some gram-negative organisms
Treats atypicals such as Legionella pneumonia, pertussis, diphtheria, andpneumonia caused by Mycoplasma pneumoniae
Can be used as an alternative to PCN in allergic individuals
Adverse EffectsGI effects, liver injury
Inhibitor of cytochrome P450Increases levels of theophylline, carbamazepine, and some statins
ERYTHROMYCINCLARITHROMYCIN (BIAXIN)
AZITHROMYCIN (ZITHROMAX)DIRITHROMYCIN (DYNABAC)
TELITHROMYCIN (KETEK)
Macrolide AntibioticsBroad-Spectrum Antibiotics
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CLINDAMYCIN (CLEOCIN)Antibiotic
Inhibits bacterial protein synthesis
UsesActive against most anaerobic bacteria outside the CNS
Bacteroides fragilis, Fusobacterium, Clostridium perfringens
Adverse EffectsAntibiotic-associated pseudomembranous colitis (AAPMC)
Diarrhea
CLINDAMYCIN (CLEOCIN)
Antibiotic
GENTAMICIN (GARAMYCIN)Aminoglycoside Antibiotic
Narrow-Spectrum Antibiotic
Disrupts bacterial protein synthesis
UsesEffective against aerobic gram-negative bacilli
Adverse EffectsNephrotoxicity (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
GENTAMICIN (GARAMYCIN)AMIKACIN (AMIKIN)
TOBRAMYCIN (NEBCIN)
Aminoglycoside AntibioticsNarrow-Spectrum Antibiotics
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TRIMETHOPRIM/SULFAMETHOXAZOLE (TMP-SMZ-BACTRIM)
Antibiotic
Combination antibiotic that inhibits bacterial synthesis of folic acid
UsesUrinary tract infections
Pneumonia caused by Pneumocystis carinii
Adverse EffectsNausea, vomiting, rash, blood dyscrasias
Hypersensitivity reactions (Stevens-Johnson syndrome)Not for use in patients with sulfa allergiesAvoid use in pregnant women near term
Avoid use in infants under the age of 2 months
TRIMETHOPRIM/SULFAMETHOXAZOLE (TMP-SMZ-BACTRIM)
Antibiotic
CIPROFLOXACIN (CIPRO)Fluoroquinolone Antibiotic
Inhibits bacterial DNA
UsesInfections of the urinary, respiratory, and GI tracts; bones; joints; skin;
and soft tissues
Adverse EffectsGI upset, CNS effects (dizziness, headache, restlessness)
Achilles tendon ruptureDo not take with milk products
Elevates levels of warfarinNot recommended for children under 18 years old
Avoid in pregnancy
CIPROFLOXACIN (CIPRO)MOXIFLOXACIN (AVELOX)GATIFLOXACIN (TEQUIN)
LEVOFLOXACIN (LEVAQUIN)
Fluoroquinolone Antibiotics
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METRONIDAZOLE (FLAGYL)Antibacterial Drug
Causes cell death by damaging bacterial DNA
UsesProtozoal infection
Infections caused by obligate anaerobic bacteriaBacteroides, Clostridium difficile, Helicobacter pylori, Trichomonas
vaginalis, giardiasisUsed as prophylaxis in colorectal or abdominal surgery
Adverse EffectsNausea, headache, dry mouth, metallic taste
Dark discoloration of urineDisulfiram-like effect when used with alcohol
Increases warfarin levels
METRONIDAZOLE (FLAGYL)
Antibacterial Drug
KETOCONAZOLE (NIZORAL)Antifungal Agent
Causes bacterial cell wall to leak
UsesSystemic and superficial mycoses (fungi)
Adverse EffectsHepatotoxicity (monitor liver function tests [LFTs])
Decreases sex hormonesDon’t give with PPIs
Inhibits hepatic drug-metabolizing enzymesIncreases levels of warfarin, phenytoin, and some statins
KETOCONAZOLE (NIZORAL)FLUCONAZOLE (DIFLUCAN)
ITRACONAZOLE (SPORANOX)MICONAZOLE (MONISTAT)
CLOTRIMAZOLE
Antifungal Agents
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Copyright © 2007 by Saunders, an imprint of Elsevier Inc.
GRISEOFULVINAntifungal Agent
Inhibits fungal mitosis
UsesSuperficial mycoses (fungi)
Dermatophytic infections of the skin, hair, and nailsNot active against Candida species or systemic mycoses
May take 3 to 8 weeks to respond
Adverse EffectsMay decrease the effects of warfarin
GRISEOFULVIN
Antifungal Agent
ACYCLOVIR (ZOVIRAX)Antiviral Agent
Suppresses synthesis of viral DNA
UsesHerpesvirus, varicella-zoster virus, cytomegalovirus (CMV)
Adverse EffectsIV administration can lead to phlebitis and nephrotoxicity
Infuse slowly over 1 hour and maintain hydrationOral therapy may lead to nausea, vomiting, diarrhea
Headache and vertigo
ACYCLOVIR (ZOVIRAX)VALACYCLOVIR (VALTREX)
FAMCICLOVIR (FAMVIR)
Antiviral Agents
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INTERFERON ALPHAAntiviral Agent
Decreases viral replication
UsesHepatitis B and C
Adverse EffectsFlulike syndrome
DepressionFatigue, hair loss, thyroid damage, heart damage
Bone marrow suppression
INTERFERON ALPHA
Antiviral Agent
RIBAVIRIN (REBETOL)Antiviral Agent
UsesUsed with interferon for treatment of hepatitis C
Adverse EffectsHemolytic anemia
Fetal harm (Category X)Use second reliable form of birth control during treatment and 6 months
after treatment
RIBAVIRIN (REBETOL)
Antiviral Agent
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Copyright © 2007 by Saunders, an imprint of Elsevier Inc.
NUCLEOSIDE REVERSE TRANSCRIPTASEINHIBITORS (NRTIs)Antiretroviral Drugs
Suppress the synthesis of viral DNA by blocking transcriptase
UsesHIV infection
Adverse EffectsAnemia, neutropenia, lactic acidosis
NUCLEOSIDE REVERSE TRANSCRIPTASEINHIBITORS (NRTIs)
Zidovudine (Retrovir)Lamivudine (Epivir)Zalcitabine (Hivid)
Antiretroviral Drugs
NON-NUCLEOSIDE REVERSE TRANSCRIPTASEINHIBITORS (NNRTIs)Antiretroviral Drugs
Inhibit reverse transcriptase by binding to it
UsesHIV infection
Adverse EffectsRash, Stevens-Johnson syndrome, erythema multiforme
Hepatotoxicity
NON-NUCLEOSIDE REVERSE TRANSCRIPTASEINHIBITORS (NNRTIs)
Delavirdine (Rescriptor)Efavirenz (Sustiva)
Nevirapine (Viramune)
Antiretroviral Drugs
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PROTEASE INHIBITORSAntiretroviral Drugs
Inhibit the enzyme protease, needed for HIV to mature
UsesHIV
Adverse EffectsHyperglycemia, diabetes, fat redistribution, hyperlipidemia
Increased bleeding in hemophiliac patientsReduced bone mineral density
Elevation of serum transaminasesCan increase or decrease levels of other drugs
PROTEASE INHIBITORSNelfinavir (Viracept)Ritonavir (Norvir)
Saquinavir (Invirase)
Antiretroviral Drugs