Pharmacology Flash Cards

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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

Continued

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

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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


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


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


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


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


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


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


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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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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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)


UsesTreats infections caused by Haemophilus influenzae, Escherichia coli,

Proteus mirabilis, enterococciNeisseria gonorrhoeae

Adverse EffectsDiarrhea

AMOXICILLIN (AMOXIL)

Broad-Spectrum Penicillin (Aminopenicillin)

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CEFAZOLIN (KEFZOL, ANCEF)First-Generation Cephalosporin

Beta-Lactam Antibiotic


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



UsesUpper respiratory tract infections

Acute otitis media (AOM) and sinusitis




CEFUROXIME (CEFTIN)

Second-Generation CephalosporinBeta-Lactam Antibiotic

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CEFTRIAXONE (ROCEPHIN)Third-Generation Cephalosporin



UsesActive against gram-negative organisms




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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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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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)


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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)


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