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259 Cards in this Set

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Autonomics:

Side effects include cycloplegia, flushing, confusion, increased body temperature, dry mouth, tachycardia, and constipation
Atropine

[The side effects of this competitive muscarinic antagonist, as well as for all anticholinergics, are remembered as blind as a bat, red as a beet, mad as a hatter, hot as a hare, and dry as a bone.]
Autonomics:

Muscarinic agonist used to treat postoperative urinary retention and atonic ileus
Bethanechol

[A related drug, carbachol, has both muscarinic and nicotinic agonist properties and is primarily used in the management of glaucoma. Both drugs are resistant to metabolism by acetylcholinesterases.]
Autonomics:

Short-acting anticholinesterase used to distinguish the diagnosis of myasthenia gravis from cholinergic crisis.
Edrophonium

[Intravenous injection of this rapidly absorbed drug results in an appreciable increase in muscle strength.]
Autonomics:

Indirect-acting sympathomimetic used in over-the-counter nasal decongestants
Ephedrine

[It has many of the same actions as amphetamines, with less central nervous system [CNS] stimulation; it is found in Chinese herbs such as ma-huang; one enantiomer, pseudoephedrine, is found in many cold-relief medications.]
Autonomics:

Adrenergic agonist used for acute asthma, anaphylactic shock, open-angle glaucoma, and cardiac resuscitation
Epinephrine

[Adrenergic agonist with affinity for α₁, α₂, β₁, and β₂ receptors. At low concentrations the effects of the β receptors predominate. β₂ receptors cause vasodilation with decreased total peripheral resistance (TPR) and decreased diastolic pressure. At higher concentrations, β₁ receptors lead to increased cardiac contractility and increased heart rate.]
Autonomics:

Prototypic β agonist used for the treatment of both acute heart failure and acute asthma
Isoproterenol

[This agent has equivalent affinities for β₁ and β₂ receptors; the β₁ activity causes an increase in cardiac contractility and increased heart rate, resulting in increased stroke volume and cardiac output; the β₂ activity induces bronchodilation.]
Autonomics:

Adregenergic antagonist used in the management of hypertension caused by pheochromocytoma; this agent is also used in the treatment of benign prostatic hyperplasia (BPH) but seldom for it's unfavorable side effects
Phenoxybenzamine

[An irreversible α₁ and α₂ antagonist; a similar short-acting reversible antagonist, phentolamine, is used in the diagnosis of pheochromocytoma.]
Autonomics:

Used in emergency situations for the treatment of both open- and narrow-angle glaucoma
Pilocarpine

[Activation of muscarinic cholinergic receptors causes contraction of the ciliary muscles with opening of Schlemm's canal, allowing drainage of aqueous humor and a subsequent decrease in intraocular pressure.]
Autonomics:

Used to treat hypertension and urinary retention; first-dose syncope is a significant side effect associated with this drug
Prazosin

[A competitive α₁ antagonist. The use of this drug can lead to postural hypotension, inhibition of ejaculation, reflex tachycardia, nasal congestion, and miosis.]
Autonomics:

Prototypical β antagonist used in the treatment of hypertension, glaucoma, migraines, and angina; as prophylaxis for myocardial infarctions; and at low doses to prevent performance anxiety
Propanolol

[Nonselective β₁ and β₂ blocker, not to be used in patients with chronic obstructive pulmonary disease (COPD) and asthma, due to significant bronchoconstriction.]
Autonomics:

Long-acting anticholinesterase used in the chronic treatment of myasthenia gravis
Pyridostigmine

[Also used as an antidote to tubocurarine toxicity; neostigmine is a similar substance, although it has a shorter duration of action.]
Autonomics:

Used to prevent motion sickness and delivered by a transdermal patch
Scopolamine

[Competitive cholinergic antagonist with sedating and amnestic effects.]
Autonomics:

Depolarizing neuromuscular blocker used to facilitate intubation, and as a skeletal muscle relaxant for general anesthesia
Succinylcholine

[Functions as a cholinergic nicotinic agonist, facilitating the opening of sodium channels. A rare but significant side effect, malignant hyperthermia, can occure in some patients when used with halothane.]
Autonomics:

Nondepolarizing neuromuscular ganglionic blockers used in surgical anesthesia
Tubocurarine
Pancuronium
Muvacurium

[Neostigmine, physostigmine, and edrophonium can reverse the paralysis caused by these drugs. Tubocurarine is the most likely of this class to cause the release of histamine, leading to vasodilation and hypotension.]
Diuretic used in the management of chronic glaucoma and acute mountain sickness; also used to alkalinize the urine in aspirin toxicity
Acetazolamide

[Inhibits carbonic anhydrase in the proximal convoluted tubule; metabolic acidosis is a potential side effect.]
Potassium-sparing diuretics that do not have anti-androgenic effects
Amiloride
Triamterene

[Block sodium channels in the cortical collecting tubules; may cause hyperkalemic metabolic acidosis]
Cough is a major side effect of this group of antihypertensive drugs
ACE Inhibitors
(Captopril/Enalapril/Lisinopril)

[Inhibit the conversion of angiotensin I to angiotensin II; inhibit breakdown of bradykinin, resulting in cough and potent vasodilation]
Most potent class of diuretics that inhibit the Na⁺/K⁺/Cl⁻ cotransporter in the thick ascending loop of Henle
Loop diuretics
(Furosemide/Butamide)

[These sulfa drugs can cause hypercalcemia, ototoxicity, hyperuricemia, hypokalemia, and metabolic alkalosis; ethacrynic acid is a non-sulfa drug with similar effects]
Diuretic that functions early in the distal convoluted tubule by inhibiting NaCl reabsorption
Hydrochlorothiazide (HCTZ)

[Major side effects include hypokalemia, alkalosis, hyperuricemia, and hyperlipidemia]
Angiotensin II receptor antagonist used as an antihypertensive drug
Losartan

[Functions at the collecting tubules, like ACE inhibitors, but no cough as side effect. Again, like ACE inhibitors, this drug is teratogenic and, therefore, contraindicated during pregnancy.]
Osmotic diuretic that works by extracting water from tissues into the blood; used in the treatment of hydrocephalus and increased intracranial pressure]
Mannitol

[This diuretic functions primarily within the proximal convoluted tubules and is used to maintain high urine output in cases of severe hemolysis or rhabdomyolysis]
This potassium-sparing diuretic is an aldosterone antagonist that functions at the collecting tubule
Spironolactone

[Increases P450 activity and causes gynecomastia and other antiandrogenic effects]
Originally developed as an antihypertensive agent, it is used topically because of the beneficial side effect of hypertrichosis
Minoxidil

[Functions as a direct-acting vasodilator, as do nitroprusside and hydralazine]
This diuretic is a potent vasodilator used in the treatment of malignant hypertension, but can cause significant postural hypotension
Nitroprusside

[Functions to stimulate guanyl cyclase with an increase in cGMP within smooth muscle of the vasculature. Prolonged infusion can result in cyanide poisoning due to release of CN⁻.]
Cardiovascular:

Extremely short-acting agent (15-20 seconds) administered IV for the control of atrioventricular (AV) nodal arrhythmias
Adenosine

[The side effects of flushing and hypotension are short-lived as well, and do not limit the use of this agent]
Cardiovascular:

Long-acting class II antiarrhythmic associated with pulmonary fibrosis, thyroid dysfunction, and corneal microdeposits
Amiodarone

[This agent also blocks sodium channels, such as the class IA antiarrhythmics]
Cardiovascular:

Used for the treatment of congestive heart failure, this agent contains two isomers, one with nonselective β blocking activity and one with α₁ blocking activity
Carvedilol

[Labetolol has similar properties and has four diastereomers; the RR enantiomer is a nonselective β blocker, and the SR enantiomer is an α₁ blocker]
Cardiovascular:

Bile acid-binding resins used in the management of hyperlipidemia
Cholestyramine
Colestipol

[Bind bile acids, preventing enterohepatic recycling, thus diverting hepatic efforts to renew bile acids, instead of producing plasma lipids]
Cardiovascular:

These agents function to slow conduction velocity by slowing the rate and rise of the action potential
Class IA Antiarrhythmics
(Quinidine/Procainamide/Disopyramide)

[These agents help maintain sinoatrial (SA) rhythm after cardioconversion for atrial fibrillation, and may cause torsade de pointes arrhythmias. Quinidine may cause cinchonism, a type of poisoning that causes headache, vertigo, and tinnitus.]
Cardiovascular:

Function to decrease the action potential duration by shortening the repolarization phase
Class IB Antiarrhythmics
(Lidocaine/Mexiletine/Tocainide/Phenytoin)

[These agents are used for the treatment of ventricular arrhythmias, as well as for digitoxin-induced arrhythmias]
Cardiovascular:

Used for the treatment of refractory ventricular arrhythmias, as well as for rapid atrial arrhythmias associated with Wolff-Parkinson-White syndrome
Class IC Antiarrhythmics
(Flecainide/Propafenone)

[Function to slow conduction velocity in the atrial and ventricular cells but do not affect the action potential. They typically are used as a last resort, as their use is associated with drug-induced arrhythmias.]
Cardiovasculae:

These agents decrease the automaticity of the pacemaker tissue of the heart, resulting in prolonged atrioventricular (AV) conduction and slower heart rate
Class II Antiarrhythmics
(Propanolol/Esmolol)

[These β blockers decrease cAMP levels, resulting in reduced sodium and calcium currents. These agents are not to be used in cases of congestive heart failure.]
Cardiovascular:

Used for the treatment of recurrent ventricular arrhythmias; many of these agents can precipitate torsade de pointe arrhythmias
Class II Antiarrhythmics
(Sotalol/Ibutilide/Bretylium/Amiodarone)

[These agents prolong the action potentials by blocking potassium channels.]
Cardiovascular:

Used for atrial arrhythmias and nodal re-entry, as well as hypertension and angina, these agents inhibit Ca⁺2 voltage channels
Class IV Antiarrhythmics
(Verapamil/Diltiazem)

[Note: nifedipine has a similar mechanism of action, but it is used only for hypertension and angina; as it has no effect on heart tissue, it is not a class IV agent]
Cardiovascular:

Centrally-acting α₂ agonist that reduces sympathetic autonomic nervous system outflow, resulting in decreased blood pressure
Clonidine

[A major side effect of this drug is rebound hypertension, in the event of abrupt discontinuation]
Cardiovascular:

Used in the management of congestive heart failure, these drugs are reversible inhibitors of Na⁺/K⁺ ATPase
Digitoxin
Digoxin

[Unlike digitoxin, digoxin is shorter-acting and excreted by the kidneys; patients with low K⁺, low Mg⁺2, high Na⁺, or high Ca⁺2 can experience arrhythmias with either agent]
Cardiovascular:

Agents that decrease triglycerides dramatically by stimulating lipoprotein lipase
Gemfibrozil
Fenofibrate
Clofibrate

[Clofibrate has been associated with gallstones and hepatobiliary neoplasms]
Cardiovascular:

Antihypertensive drug that blocks the release of norepinephrine by displacing it from intracellular vesicles
Guanethidine

[Side effects include serious orthostatic hypotension; the effects of the drug are antagonized by tricyclic antidepressants]
Cardiovascular:

Used for the treatment of ventricular arrhythmias, especially following myocardial infarction, because it works only on ischemic tissue
Lidocaine

[This class IB antiarrhythmic has little effect on the ECG of normal (nonischemic) heart tissue. It is given intravenously, although similar agents (mexiletine and tocainide) are given orally.]
Cardiovascular:

This α₂ agonist decreases adrenergic outflow from the CNS, resulting in decreased peripheral resistance and decreased blood pressure
Methyldopa

[This drug can haptenate red blood cell proteins, resulting in autoimmune hemolytic anemia]
Cardiovascular:

Lipid-lowering agent that causes cutaneous flushing, which can be avoided by administering concurrently with aspirin
Niacin

[Directly reduces the secretion of VLDLs from and apolipoprotein synthesis by the liver, while increasing HDLs]
Cardiovascular:

Causes an increase in cGMP within vascular smooth muscle, resulting in decreased preload to the heart and decreased blood pressure
Nitroglycerin

[Administered as a sublingually to decrease first-pass metabolism; potential side effects include cyanide poisoning, postural hypotension, headache, and flushing]
Cardiovascular:

Antihyperlipidemic agent that may prevent atherosclerosis by acting as an antioxidant
Probucol

[Rarely used for the treatment of hyperlipidemia because it decreases HDLs as well as LDLs; may be efficacious in preventing restenosis after angioplasty]
Cardiovascular:

This rarely used antihypertensive agent blocks the storage and release of catecholamines and serotonin from neurons
Reserpine

[This drug readily enters the CNS and can cause suicidal depression and Parkinsonian symptoms]
Cardiovascular:

Inhibit the rate-limiting enzyme of cholesterol synthesis, HMG-CoA reductase, resulting in dramatically decreased LDL levels
Statins
(Lovastatin/Pravastatin/Simvastatin/Atorvastatin)

[May cause elevated liver enzymes, myositis with increased creatinine kinase from skeletal muscle, and rarely, rhabdomyolysis]
CNS:

Intermediate-acting benzodiazepine used for the treatment of panic disorder and phobias
Alprazolam

[Both alprazolam and clonazepam have sedative effects and can cause physiologic dependence; buspirone is an alternative drug that binds 5-HT1A receptors with minimal abuse potential]
CNS:

Used in the management of depression, it inhibits the reabsorption of both norepinephrine and serotonin within the synapse
Amitriptyline

[Other tricyclic antidepressants include nortryptyline, imipramine, and despiramine. Major side effects of this class include sedation, orthostatic hypotension, and cardiac arrhythmias.]
CNS:

Orally active antispasmolytic agent
Baclofen

[GABA receptor agonist that functions on inhibitory pathways in the spinal cord]
CNS:

Because of its low toxicity, this local anesthetic can be used on large surface areas and is available over the counter as an ointment
Benzocaine

[This ester-type compound, like cocaine, has surface activity, or the ability to work on superficial nerves when applied to mucous membranes. Other ester-type compounds include the short-acting procaine and the long-acting tetracaine.]
CNS:

This antimuscarinic is used in the management of Parkinson disease, improving tremors and rigidity, but does little for bradykinesia
Benztropine

[As for all antimuscarinics, contraindications include prostatic hyperplasia, GI obstruction, and closed-angle glaucoma, and are more common in older patients]
CNS:

Drug used in the treatment of Parkinson disease as well as in the treatment of prolactinoma
Bromocriptine

[This ergot derivative acts as a D2 agonist, improving extrapyramidal function, and also inhibits the release of prolactin from the pituitary gland. Unlike a similar agent, pergolide, bromocriptine maintains its effectiveness over time.]
CNS:

This long-acting amide-type local anesthetic can cause severe hypotension and arrhythmias if inadvertently given intravenously
Bupivacaine

[Local anesthetics bind to sodium channels in the open and inactive state, slowing recovery from depolarization 10- to 1000-fold]
CNS:

Antidepressant used in the management of nicotine withdrawal in patients seeking to stop cigarette smoking with minimal sedation
Bupropion

[This second-generaltion heterocyclic antidepressant inhibits the reuptake of norepinephrine. Newere third-generation agents used for depression, such as venlafaxine, inhibit the reuptake of serotonin as well.]
CNS:

This agent is used in the treatment of partial and generalized seizures, bipolar disorder, and is the primary agent used in the treatment of trigeminal neuralgia
Carbamazepine

[Inhibits sodium channels on neurons; it's use may result in idiosyncratic blood disorders such as aplastic anemia and agranulocytosis]
CNS:

Second-line treatment for schizophrenia that is better for the negative symptoms of the disease
Clozapine

[Atypical antipsychotic, associated with agranulocytosis, that blocks the D4 receptor]
CNS:

The only local anesthetic with vasoconstrictor activity, but is rarely used
Cocaine

[Has been widely replaced with the use of synthetics such as benzocaine and proparacaine. Other local anesthetics are administered with epinephrine to increase the duration of action and lower the effective dose.]
CNS:

Used for the treatments of anxiety and ethanol dependence; also a primary agent in the treatment of status epilepticus
Diazepam

[This long-acting, prototypic benzodiazepine binds to the GABA-A receptor, increasing the frequency of chloride channel opening]
CNS:

Used in the treatment of Parkinson's disease, it inhibits the enzyme catechol-O-methyltransferase (COMT)
Entacapone

[This agent inhibits the conversion of levodopa to 3-O-methyldopa in the periphery. A similar agent, tolcapone, has been associated with acute liver failure.]
CNS:

Preferred agent in the treatment of absence seizures
Ethosuximide

[Postulated to function by inhibiting T-type calcium channels in thalamic neurons. Use has been associated with the development of Stevens-Johnson syndrome.]
CNS:

Opioid used in the induction of anesthesia, and also for postoperative analgesia
Fentanyl

[If used in conjunction with droperidol and nitrous oxide, it can produce a state of neuroleptanesthesia, resulting in both analgesia and amnesia]
CNS:

Popular drug used for the treatment of depression, it is the prototype of the selective serotonin reuptake inhibitors (SSRI)
Fluoxetine

[Common side effects of this and other SSRI's, such as sertraline, paroxetine, and citalopram, include headache, insomnia, nausea, and sexual dysfunction; these agents also are used in the management of obsessive compulsive disorder (OCD), social phobias, bulimia, and alcohol dependence]
CNS:

This analog of GABA is used in the treatment of partial seizures, as well as in the management of peripheral neuropathy
Gabapentin

[Other available agents for seizures include lamotrigine, which may cause life-threatening Stevens-Johnson syndrome and epidermal necrolysis, and vigabatrin, which inhibits GABA transaminases]
CNS:

The most potent inhaled halogenated anesthetic, with the lowest minimal alveolar concentration (MAC), but now rarely used for surgical anesthesia in children and asthmatics
Halothane

[The use of halothane has been largely replaced by isoflurane, sevoflurane, and desflurane. Rare but significant side effects include the development of malignant hyperthermia and fulminant hepatitis]
CNS:

Dissociative anesthetic that causes hallucinations and disorientation on recovery
Ketamine

[Side effects are due to an increase in cerebral blood flow, and can be reduced by preoperative use of benzodiazepines]
CNS:

Used in the treatment of Parkinson's disease, this precursor crosses the blood-brain barrier and is converted to dopamine
L-dopa (Levodopa)

[Administered with the decarboxylase inhibitor carbidopa (which does not cross the blood-brain barrier) to increase bioavailability and to limit peripheral side effects]
CNS:

Mood stabilizer that is a first-line drug for the treatment of bipolar affective disorder
Lithium

[Inhibits the secondary messengers inositol triphosphate (IP3) and diacylglycerol (DAG) and causes tremor, hypothyroidism, polydipsia, and polyuria]
CNS:

Amphetamine used in the management of attention deficit disorder (ADD) and narcolepsy
Methylphenidate (Ritalin, Concerta)

[Increases alertness and decreases appetite by stimulating the release of catecholamines; it is a controlled substance with abuse potential]
CNS:

Inhaled anesthetic that never reaches the level of surgical anesthesia without the addition of another agent, it is safe and the induction and recovery are extremely rapid
Nitrous Oxide

[This gas has a high minimal alveolar concentration (MAC) and a low blood/gas partition. It is usually administered with an intravenous anesthetic such as thiopental, and is commonly used in dental procedures.]
CNS:

This older agent used in the treatment of depression increases levels of amine neurotransmitters by inhibiting their breakdown
Monoamine oxidase inhibitors (MAOI)
(Phenelzine/Tranylcyromine/Isocarboxazid)

[Consumption of foods such as cheese, which contain tyramine (an indirect-acting sympathomimetic) while on MAOIs can result in hypertensive crisis. If taken with selective serotonin reuptake inhibitors (SSRIs), life threatening serotonin syndrome can result.]
CNS:

Used as a sedative; also us a first-line drug for tonic-clonic seizures in children and in the treatment of patients with Crigler-Najjar syndrome type II
Phenobarbital

[As a long-acting, prototypic barbituate, it binds to GABA receptors, increasing the duration of chloride channel opening with neuronal inhibition]
CNS:

Drug used for the treatment of partial and tonic-cloninc seizures and status epileptics, as well as being a class IB antiarrhythmic
Phenytoin

[Side effects include gigival hyperplasia, hirsutism, anemia, and birth defects, because it interferes with folate absorption]
CNS:

This agent has the largest number of extrapyramidal side effects of all the atypical antipsychotics
Risperidone

[Atypical antipsychotics block the D2 and the 5-HT2 receptors, contributing to high sedation. More recently introduced agents such as olanzapine have no extrapyramidal effects]
CNS:

Agent used in the treatment of Parkinson's disease that forestalls the use of levodopa
Ropinirole

[This agent has a lower incidence of postural hypertension, dyskinesia, vomiting, and hallucination, unlike most dopamine agonists. It is not an ergot derivative; a similar agent, pramipexole, also is used]
CNS:

Inhibits the degradation of dopamine in the central nervous system and is used as an adjuvant to levodopa in the treatment of Parkinson's disease
Selegiline

[Inhibits monoamine oxidase B, which selectively degrades dopamine]
CNS:

Ultra-short-acting barbituate used intravenously for the induction of surgical anesthesia
Thiopental

[Due to its high lipid solubility, this agent enters the CNS within 1 minute; it can be used only for short surgical procedures, because it rapidly redistributes to other tissues]
CNS:

Side effects of this antipsychotic include torsade de pointes arrhythmias and retinal deposits
Thioridazine

[This low-potency antipsychotic blocks most dopamine receptors in the CNS, and can cause postural hypotension, sedation, and CNS depression]
CNS:

Used in the treatment of most forms of epilepsy, including generalized tonic-clonic, partial, absence, and myoclonic seizures, and in the treatment of bipolar disorder
Valproic Acid

[This agent has been associated with the development of neural tube defects when administered to pregnant women]
CNS:

Although not a benzodiazepine, it has similar effects and is used as a hypnotic with less dependence liability
Zolpidem

[Functions by binding to benzodiazepine (BDZ) receptors and thus results in similar actions with less amnesia and less muscle relaxation; also like benzodiazepines, its actions are antagonized by flumazenil]
Drugs of Abuse:

Causes feelings of euphoria and self-confidence, and, at chronic high doses, delusions and paranoia
Amphetamines

[Function as indirect sypathomimetic by releasing stored catecholamines]
Drugs of Abuse:

Overdose often results in fatalities from arrhythmias, myocardial infarctions, or seizures
Cocaine

[Inhibits catecholamine reuptake, resulting in cardiotoxicity and hypertensive episodes]
Drugs of Abuse:

Used in the treatment of alcoholism in compliant patients, causing flushing, vomiting, and hypertension when alcohol is consumed
Disulfram

[Inhibits aldehyde dehydrogenase, resulting in the toxic accumulation of acetaldehyde. Drugs with similar side effects are said to cause a disulfram-like reaction.]
Drugs of Abuse:

Congener of amphetamine that results in increased intrapersonal communications and increased sexual drive
Ecstasy

[Methylene dioxymethamphetamine (MDMA) use is often associated with "rave" parties and in teenagers of higher socioeconomic status]
Drugs of Abuse:

Rapidly acting benzodiazepine used as a "date-rape" drug
Flunitrazepam (Rohypnol)

[Due to its amnestic properties, this drug often is added to alcohol, making the victim incapable of resisting or remembering being raped]
Drugs of Abuse:

Hallucinogenic agent that causes "psychedelic" perceptual effects and can lead to a "bad trip" or panic attack
Lysergic Acid Diethylamide (LSD)

["Highs" also are associated with somatic effetcs, such as nausea, parethesias, and weakness; such effects are also seen with the use of mescaline and psilocybin]
Drugs of Abuse:

"High" is associated with euphoria, disinhibition, laughter, changes in perception, and hunger
Marijuana

[The active ingredient, tetrahydrocannabinol (THC), can be used medically to lower intraocular pressure in glaucoma]
Drugs of Abuse:

Used in the management of opioid withdrawal and maintenance programs for addicts
Methadone

[Used to treat the nausea, chills, sweats, lacrimation, cramps, rhinorrhea, yawning, piloerection, diarrhea, and tremor due to opioid withdrawal]
Drugs of Abuse:

A by-product of incorrectly synthesized illicit street opioids, this contaminant can cause irreversible parkinsonism
MPTP (I-methyl-4-phenyl-1,2,3,6-tetrahydropyridine)

[Causes the destruction of dopaminergic neurons of the nigrostriatal tract]
Drugs of Abuse:

Overdose causes constricted pupils, clammy skin, nausea, drowsiness, and respiratory depression with possible coma and death
Opioids
(Heroin/Morphine/Meperidine/Fentanyl)

[Modulate synaptic transmission by binding mu (morphine), delta (enkephalin), and kappa (dynorphin) receptors]
Drugs of Abuse:

Hallucinogen that often causes psychotic reactions and impaired judgement leading to reckless behavior
Phencyclidine (PCP)

[Also known as "angel dust"; overdose leads to nystagmus, life-threatening hypertension, and seizures]
Anti-Inflammatory:

Commonly used analgesic and antipyretic, but unlike NSAIDs, has no anti-inflammatory properties
Acetaminophen

[Weak inhibitor of cyclooxygenase (COX), it inhibits prostaglandin synthesis in the central nervous system; a related prodrug, phenacetin, is no longer available due to nephrotoxicity]
Anti-Inflammatory:

Used in the management of chronic gout and as an adjunct to cancer chemotherapy, to slow the production of uric acid
Allopurinol

[Results in suicide inhibition of xanthine oxidase with resultant increase of xanthine and hypoxanthine, both of which are more soluble and less likely to form crystals than uric acid]
Anti-Inflammatory:

Nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, antiplatelet, and anti-inflammatory properties that irreversibly inhibits cyclooxygenase
Aspirin (acetylsalicylic acid)

[Inhibits the formation of prostaglandin E (PGE), decreases pain and fever, and decreases the synthesis of PGE in the stomach, predisposing to acute gastritis]
Anti-Inflammatory:

Used topically for the treatment of rheumatoid arthritis because it depletes substance P
Capsaicin

[Component of chili peppers that impairs the release of substance P, the potent neurotransmitter for pain sensation]
Anti-Inflammatory:

NSAID used in the treatment of rheumatoid arthritis and other chronic conditions, with a decreased risk of ulcers and other GI bleeds
Celecoxib

[Celecoxib and a similar drug, rofecoxib, selectively inhibit cyclooxygenase-2 (COX-2) present only in leukocytes; these agents do not inhibit COX-1 that produces protective prostaglandins in the stomach; as sulfa drugs, they both can cause hypersensitivity in some patients]
Anti-Inflammatory:

Used for the treatment of acute attacks of gouty arthritis, because it impairs leukocyte function
Colchicine

[Inhibits microtuble assembly, and therefore, leukocyte migration and phagocytosis of uric acid crystals]
Anti-Inflammatory:

Used in the treatment of transplant patients and patients with autoimmune diseases, as it impairs T cell production of interleukin-2 (IL-2)
Cyclosporin

[Binds to cyclophilins and inhibits the transcription of cytokine genes; a similar agent, tacrolimus, binds to the immunophilin FK-binding protein (FKBP) and functions similarly; both display dose-limiting nephrotoxicity]
Anti-Inflammatory:

Monoclonal antibody used in the management of patients with renal allografts
Daclizumab

[Binds to the high affinity interleukin-2 (IL-2) receptor expressed on activated T cells; the side effects are minimal compared to agents such as cyclosporin or tacrolimus]
Anti-Inflammatory:

Used in the treatment of rheumatoid arthritis and inflammatory bowel disease, a recombinant protein that inhibits the effects of tumor necrosis factor alpha (TNF-α)
Etanercept

[Administered IV this drug is a fusion between the extracellular domain of the TNF-α receptor and the Fc portion of an antibody; a similar monoclonal antibody, infliximab, also binds and inhibits TNF-α]
Anti-Inflammatory:

Drug used in the treatment of severe rheumatoid arthritis, because it decreases lysosomal and macrophage function
Gold salts

[Side effects include dermatitis, hematotoxicity, and nephrotoxicity]
Anti-Inflammatory:

Reversible inhibitors of cyclooxygenase widely used as over-the-counter pain relievers
Ibuprofen
Naproxen
Piroxicam

[These agents share many of the same side effects as aspirin, but are more efficacious analgesics and anti-inflammatories; however, they lack aspirin's long duration and antiplatelet effects]
Anti-Inflammatory:

High-potency NSAID used in the treatment of gout and arthritis, and closure of a patent ductus arteriosus
Indomethacin

[Conversly, prostaglandin E (PGE) can be used to maintain a patent ductus arteriosus in congenital cyanotic heart disease]
Anti-Inflammatory:

The only parenteral NSAID, used primarily for its analgesic (rather than anti-inflammatory) properties
Ketorolac

[Its systemic route of delivery substantially decreases GI irritation]
Anti-Inflammatory:

Unlike most opioid agonists, this derivative does not cause biliary spasms, and is preferred, therefore, as an analgesic for pancreatitis and cholecystitis
Meperidine

[Causes relaxation of the sphincter of Oddi; all opioids are contraindicated in cases of head injury, because they cause increased intracranial pressure]
Anti-Inflammatory:

Used in the prevention of headaches, this ergot derivative has no value in the treatment of acute migraine attacks
Methylsergide

[Because this agent blocks serotonin (5-HT) receptors, it can be used in the treatment of carcinoid tumors; notable side effects include retroperitoneal and subendocardial fibroplasia]
Anti-Inflammatory:

Uricosuric agent used in the treatment of chronic gout, and also to increase the effective concentration of weakly acidic drugs such as penicillins
Probenecid

[Both probenecid and sulfinpyrazone compete with uric acid for reabsorption in the proximal tubules of the kidney, and also inhibit the secretion of weak acids]
Anti-Inflammatory:

Given to Rh-negative mothers within 72 hours of giving birth to an Rh-positive child, to prevent the development of hemolytic disease of the newborn (erythroblastosis fetalis) in subsequent Rh-positive pregnancies
RhoGAM

[Fetal Rh-positive red blood cells that enter the maternal circu;ation are opsonized by these antibodies against the Rh (D) antigen, preventing the mother from producing anti-Rh antibodies]
Anti-Inflammatory:

Serotonin agonist used in the treatment of acute migraines and cluster headaches
Sumatriptan

[Binds to the HT1d receptor, causing vasoconstriction of the cerebral vasculature]
Anti-Inflammatory:

Notorious for causing teratogenic effects, such as phocomelia ("flipper limbs"); has gained attention as a potent immunosuppressant
Thalidomide

[Used in the treatment of systemic lupus erythematosus (SLE), multiple myeloma, and leprosy, its effects are due to its ability to suppress the production of tumor necrosis factor alpha (TNF-α)]
Blood:

Monoclonal antibody used as an anticoagulant, preventing restenosis after coronary angioplasty
Abciximab

[Antibodies against the glycoprotein IIb/IIIa receptor on platelets, preventing platelet aggregation]
Blood:

Used in the treatment of acute bleeding in patients with hemophilia and other coagulopathies
Aminocaproic acid

[An orally active inhibitor of plasminogen activation, thereby inhibiting fibrinolysis; tranexamic acid is a similar agent]
Blood:

Recombinant product used in the treatment of anemia associated with renal failure
Erythropoietin (Epoetin Alfa)

[Also used to treat anemia associated with bone marrow transplants or toxic drug reactions]
Blood:

Will correct the anemia, but not the neurologic deficits caused by vitamin B₁₂ deficiency
Folic Acid

[Vitamin B₁₂ deficiency must be ruled out before treating megaloblastic anemia with folic acid]
Blood:

Rapid-acting, intravenously administered anticoagulant, used for acute myocardial infarction and prevention of deep vein thrombosis (DVT) following prolonged immobilization
Heparin

[Binds to and activates antithrombin III, resulting in the inactivation of thrombin and other clotting factors; unlike warfarin, it does not cross the placenta and thus may be used during pregnancy. Protamine sulfate is used to reverse the effects of heparin.]
Blood:

Used in the management of sickle cell anemia, as well as for various myeloid neoplasms
Hydroxyurea

[May decrease the incidence of sickle cell crisis, by increasing levels of fetal hemoglobin (HbF); it also inhibits DNA synthesis by blocking the conversion of ribonucleotides to deoxyribonucleotide]
Blood:

Recombinantly produced granulocyte-macrophage colony-stimulating factor (GM-CSF), used in the management of patients undergoing chemotherapy
Sargramostim

[A similar agent, G-CSF (e.g., filgrastim), is used for similar applications, but affects only granulocytes]
Blood:

A bacterial product of Streptococcus pyogenes, used in the treatment of coronary artery thrombosis
Streptokinase

[Complexes with and catalyzes the conversion of plasminogen to plasmin; it is a significantly cheaper, although debatably equivalent, agent to tissue plasminogen activator (tPA)]
Blood:

Platelet antiaggregant, used for the prevention of transient ischemic attacks (TIA) in patients with aspirin sensitivity
Ticlopidine

[Interferes with the binding of fibrin to the glycoprotein IIIb/IIIa receptor on platelets]
Blood:

Created through the use of recombinant DNA technology, this agent is used for coronary artery thrombosis and ischemic stroke
Tissue Plasminogen Activator (t-PA)
(Alteplase/Reteplase)

[Converts fibrin-bound plasminogen to plasmin, resulting in dissolution of thrombi]
Blood:

Orally administered anticoagulant, used in the management and prophylaxis of venous thrombosis, myocardial infarction, and stroke
Warfarin

[Coumadin compound that interferes with the vitamin K-dependent carboxylation of clotting factors II, VII, IX, and X]
Blood:

Used for the treatment of traveler's diarrhea
Bismuth Subsalicylate

[Helps decrease fluid secretion by the bowel; also used with metronidazole and tetracycline for the treatment of Helicobacter pylori-associated peptic ulcer disease]
Gastrointestinal:

Chronic indigestion of this antacid with milk can induce milk-alkali syndrome
Calcium Carbonate

[Can result in hypercalcemic alkalosis with the development of renal calculi]
Gastrointestinal:

Used in the treatment of gastroesophageal reflux disease (GERD), this histamine blocker is associated with gynecomastia and galactorrhea
Cimetidine

[The stronger the H2 blockers, ranitidine and famotidine, do not inhibit the hepatic P450 system and, therefore, do not cause antiandrogenic effects]
Gastrointestinal:

Prokinetic agent used in the treatment of upper gastrointestinal dysfunction, such as gastroesophageal reflux disease (GERD) or gastroparesis with delayed gastric emptying
Cisapride

[Stimulates peristalsis by promoting the release of acetylcholine from postganglionic nerves of the myenteric plexus. High doses have been associated with long QT syndrome.]
Gastrointestinal:

Opioid derivatives used in the treatment of diarrhea, because they suppress gastrointestinal motility
Diphenoxylate
Loperamide

[Whereas diphenoxylate is formulated with antimuscarinic alkaloids; both preparations have minimal abuse potential]
Gastrointestinal:

This preparation is used to treat emesis and nausea associated with chemotherapy, and contains the active ingredient in marijuana
Dronabinol

[This schedule III drug, which contains tetrahydrocannabinol (THC), is a controlled substance with approved medical use and moderate potential for dependence]
Gastrointestinal:

Commonly used proemetic agent used in cases of ingestion of caustic substances or mineral oils
Ipecac Syrup

[Orally administered substance that acts directly on the chemoreceptor trigger zone in the medulla]
Gastrointestinal:

Among the most popular antacids used in the United States, neither is absorbed and, therefore, neither causes systemic effects
Magnesium Hydroxide
Aluminum Hydroxide

[Magnesium hydroxide also has a strong laxative effect, whereas aluminum hydroxide causes constipation]
Gastrointestinal:

This prokinetic agent is used to prevent emesis (e.g., post-anesthesia or due to cancer chemotherapy), because it blocks D2 receptors in the area prostrema that trigger vomiting
Metoclopramide

[Functions to facilitate acetylcholine, while antagonizing the action of dopamine on the enteric nervous system. Side effects include sedation, diarrhea, and extrapyramidal symptoms.]
Gastrointestinal:

Eicosanoid preparation used to prevent peptic ulcers in patients taking high doses of NSAIDs for conditions such as rheumatoid arthritis
Misoprostol

[This prostaglandin E (PGE) analog decreases gastric acid production and increases mucus production, protecting the lining of the stomach]
Gastrointestinal:

Proton pump inhibitor used in the treatment of gastroesophageal reflux disease (GERD), gastric and duodenal ulcers, Helicobacter pylori gastritis, and Zollinger-Ellison syndrome (gastrinoma)
Omeprazole

[Irreversibly inhibits the H⁺/K⁺ ATPase on the luminal side of parietal cells]
Gastrointestinal:

Central-acting antiemetic used to control postoperative vomiting and vomiting in chemotherapy patients
Ondansetron

[5-HT3 inhibitor that functions at the chemoreceptive area of the area postrema]
Gastrointestinal:

Used in the treatment of peptic ulcers, because it polymerizes and selectively coats necrotic ulcerated tissue
Sucralfate

[Requires an acidic environment to polymerize, and therefore, cannot be used in the presence of antacids or H2 blockers]
Respiratory:

β-adrenergic antagonists used in the treatment of hypertension for patients with asthma or chronic obstructive pulmonary disease (COPD), and smokers
Acebutolol
Atenolol
Metoprolol

[Selective β₁ blockers that decrease blood pressure, with no bronchoconstriction at low doses]
Respiratory:

Prototypic adrenergic agonist, available as an inhaler, used for the management of bronchospasm in asthmatics
Albuterol

[Other selective β₂ agonists include metaproterenol, terbutaline, and salmeterol]
Respiratory:

Synthetic glucocorticoid that readily penetrates the airway mucosa; used in the management of asthma
Beclomethasone

[Beclomethasone and a related agent, budesonide, have very short half-lives in the bloodstream, and therefore cause less systemic effects than other glucocorticoids]
Respiratory:

Stabilizes mast cell and basophil membranes, preventing the release of histamine in asthmatics
Cromolyn Sodium

[Used for prophylaxis only, not for the treatment of acute asthma attacks]
Respiratory:

Opioid agonist available in many over-the-counter cough syrups
Dextromethorphan

[Antitussive agent that depresses the cough center in the medulla; unlike dextromethorphan, codeine provides analgesia and has a higher abuse potential]
Respiratory:

Antihistaminics used for the treatment of allergic conditions (e.g., hay fever, urticaria, atopy), as well as for the treatment of motion sickness
Diphenhydramine
Chlorpheniramine

[Inhibit the binding of histamine to H1 receptors; such as older agents have anticholinergic effects, contributing to sedative side effects]
Respiratory:

Nonsedating antihistaminics used for the treatment of allergy
Fexofenadine
Loratadine

[These second-generation antihistaminics do not readily enter the CNS, preventing sedation]
Respiratory:

Aerosolized antimuscarinic agent, used in the treatment of chronic obstructive pulmonary disease (COPD) and asthma
Ipratropium

[Not as effective as β₂ agonists; dry mouth is a major side effect]
Respiratory:

Long-acting β₂ agonist used for prophylaxis of asthma
Salmeterol

[This agent works for 12 hours or more; it may cause tremors and arrhythmias]
Respiratory:

A methylxanthine used in the treatment of asthma for its bronchodilatory effects
Theophylline

[Inhibits phosphodiesterase, thereby inhibiting the degradation of cAMP to AMP; other methylxanthines include caffeine and theobromine found in cocoa]
Respiratory:

Used in the treatment of asthma, selectively inhibiting leukotriene synthesis
Zileutin

[Leukotrienes can also be inhibited by the LTD4 and LTE4 antagonists zafirlukast and montelukast]
Endocrine:

Oral hypoglycemic agent that functions within the intestinal lumen, decreasing postprandial hyperglycemia, although there are no effects on fasting sugar
Acarbose

[Inhibits α-galactosidase, an enzyme required for rapid absorption of most dietary sugars]
Endocrine:

These compounds reduce bone resorption and formation, and are used in the treatment of osteoporosis (postmenopausal, senile, or glucocorticoid-induced) and Paget's disease
Bisphosphonates
(Alendronate/Etidronate/Pamidronate/Risedronate)

[Characterized by poor oral availability and cannot be taken with food; may cause esophageal ulcerations, so must be taken with large amounts of water, and the patient must remain upright for at least 30 minutes afterward]
Endocrine:

Used in the treatment of hyperprolactinemia e.g., due to a pituitary adenoma
Bromocriptine

[Ergot alkaloid with dopaminergic activity, inhibiting the release of prolactin]
Endocrine:

Used for the treatment of osteoporosis, this hormone produced by the thyroid decreases bone breakdown, and decreases serum calcium and phosphate levels
Calcitonin

[Also used in the treatment of acute hypercalcemia and Paget's disease; salmon calcitonin is used because it is more potent and has a longer half-life; it is administered intranasally or by injection]
Endocrine:

Fertility drug used to induce ovulation in annovulatory women, although its use may be associated with multiple births
Clomiphene

[Blocks negative feedback to the pituitary, increasing the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) to stimulate ovulation]
Endocrine:

A synthetic analog adrenocorticotropin (ACTH) used to diagnose patients with abnormalities of cortisol production, e.g., Addison's disease
Cosyntropin

[Proteolytic cleavage of preproopiomelanocortin (POMC) forms ACTH and melaocyte-stimulating hormone (MSH), as well as beta-endorphin and metenkephalin]
Endocrine:

Used in the treatment of endometriosis and fibrocystic disease of the breast
Danazol

[Inhibits several P450 enzymes involved in gonadal steroid synthesis]
Endocrine:

An antidiuretic hormone (ADH) receptor agonist used for the treatment of pituitary diabetes insipidus
Desmopressin
Vasopressin

[Desmopressin is a V2-selective agonist that facilitates water reabsorption from the collecting tubules. Vasopressin is both a V1 and V2 agonist; its V1 activity increases vascular smooth muscle tone, and therefore is used in the treatment of esophageal varices.]
Endocrine:

Use of this estrogen compound by pregnant women has been associated with the development of clear cell adenocarcinoma of the vagina of their daughters
Diethylstilbestrol (DES)

[May be used as postcoital ("morning after") birth control, and for the treatment of testicular tumors
Endocrine:

Synthetic estrogen with high oral availability, used in contraceptive pills as well as in hormone replacement therapy (HRT)
Ethinyl Estradiol Mestranol

[Increasingly controversial, HRT has been shown to decrease the risk of coronary artery disease, to slow the progression of osteoporosis, and to ameliorate hot flashes in postmenopausal women; it does, however, carry a risk of breast and ovarian cancer]
Endocrine:

Antiandrogenic compound used in the treatment of benign prostatic hyperplasia and alopecia
Finasteride

[Inhibits 5α-reductase, and thus the conversion of testosterone to dihydrotestosterone (DHT]
Endocrine:

Used for mineralocorticoid deficiency, this agent has a long duration of action, and is a naturally occuring precursor to aldosterone
Fludrocortisone

[Used in conjunction with glucocorticoids in postadenalectomy therapy]
Endocrine:

This ultra-rapid-acting human insulin is administered immediately before meals
Insulin Lispro

[An altered form of insulin that enters the circulation more rapidly than crystalline zinc (regular) insulin]
Endocrine:

A synthetic thyroid hormone used in the treatment of hypothyroidism, as seen in Hashimoto's thyroiditis, myxedema, and patients on lithium
Levothyroxine (T4)

[T4 is converted in the periphery to T3, the active form of thyroid hormone. Liothyronine, synthetic T3, is faster-acting, but more expensive and, therefore is used less frequently.]
Endocrine:

Oral hypoglycemic agent that does not require functional pancreatic islet cells and decreases postprandial glucose levels without resultant hypoglycemia or weight gain
Metformin

[Biguanide compound that functions by increasing peripheral glycolysis, and therefore hepatic gluconeogenesis, resulting in a decrease in serum glucose levels]
Endocrine:

Abortifacient steroid receptor antagonist known as the "morning after" pill
Mifepristone (RU486)

[Blocks the binding of progesterone to cytoplasmic receptors, preventing successful implantation]
Endocrine:

Synthetic progesterone analog used in oral contraceptives and implantable contraceptive devices
Norgestrel

[Norgestrel and similar agents, such as norethindrone and medroxyprogesterone, may be used in hormone replacement therapy, and to prevent abnormal uterine bleeding]
Endocrine:

A synthetic analog of somatostatin, used in the treatment of many endocrine tumors, including carcinoid, gastrinoma, and somatropic pituitary ademoma
Octreotide

[This octapeptide is used instead of somatostatin, because it has a longer half-life]
Endocrine:

Normally produced in the posterior pituitary, this hormone is used to stimulate and reinforce labor, as well as stimulate milk ejection from nursing mothers
Oxytocin

[Stimulates contraction of uterine smooth muscle for labor; stimulates contraction of the myoepithelial cells of the mammary glands to eject milk]
Endocrine:

Oral agent used in the treatment of hyperthyroidism
Propylthiouracil

[Inhibits the iodination and coupling reactions in thyroid hormone synthesis. Methimazole also is used, although it can cross the placenta and enter breast milk.]
Endocrine:

This estrogen partial agonist is used to prevent osteoporosis in postmenopausal women
Raloxifene

[It also increases serum high-density lipoprotein (HDL), protecting against atherosclerosis and heart disease; unlike another selective estrogen receptor modulator (SERM), tamoxifen, it does not increase the risk of endometrial carcinoma]
Endocrine:

This insulin secretagogue has a rapid onset, but shorter duration of action, than sulfonylureas
Repaglinide

[Belongs to a class of drugs known as meglitinides, which facilitate insulin release from pancreatic β cells by binding to potassium channels]
Endocrine:

These agents increase cell sensitivity to insulin, by stimulating the peroxisomal proliferator gamma (PPARγ) nuclear receptor
Rosiglitazone
Pioglitazone

[PPARγ regulates a number of genes involved in carbohydrate metabolism, The first member of this class, troglitazone, was removed from the market because it caused hepatotoxicity]
Endocrine:

Oral hypoglycemic agents used to stimulate the release of endogenous insulin from β cells
Sulfonylureas
(Glyburide/Glipizide)

[Stimulate the closure of potassium channels, resulting in depolarization of β cells and the release of preformed insulin in vesicles]
Endocrine:

This form of insulin is given in the morning and in the evening, to maintain basal levels of insulin for 12 to 24 hours
Ultralente Insulin

[Supplemented throughout the day with Insulin Lispro; a modified version of human insulin, insuline glargine, has an even longer duration of action]
Antimicrobials:

Oral, topical, and intravenous preparations are available for this drug, used to reduce symtomatology of herpes simplex virus (HSV) infection, although it does not inhibit the reactivation of herpes
Acyclovir

[This guanosine analog is activated by the thymidine kinase of herpes viruses (including herpes simplex, varicella zoster, and Epstein-Barr) and functions as a chain terminator when incorporated into viral DNA during replication]
Antimicrobials:

Used for the prophylaxis of influenza A and rubella viral infection if given within 48 hours of exposure; also used in the treatment of Parkinson's disease
Amantadine

[A similar drug, rimantadine, has several antiviral effects with a longer half-life; both drugs inhibit the fusion of viral particles within an endosome in a cell. Amantadine is not effective against influenza B, which lacks the M2 protein to which amantadine binds.]
Antimicrobials:

Ineffective against anaerobes, due to the requirement for oxygen to be taken up by the organism
Aminoglycosides
(Gentamicin/Streptomycin/Tobramycin/Amikacin/Neomycin)

[Bactericidal inhibitors of mRNA translation at the 30S ribosome; these agents are associated with significant nephrotoxicity and ototoxicity]
Antimicrobials:

Polyene antifungal agent used for the treatment of systemic mycosis and intrathecally for the treatment of fungal meningitis
Amphotericin B

[This drug disrupts fungal membranes by binding to ergosterol, which induces pore formation. Side effects include chills, fever, hypotension, and dose-limiting nephrotoxicity, all of which are less severe when using liposomal formulations.]
Antimicrobials:

This extended-spectrum penicillin is used to treat infections with gram-negative organisms such as Haemophilus spp., E. coli, Listeria spp., Proteus spp., and Salmonella spp.
Ampicillin

[Often administered with penicillinase inhibitors; a similar drug, amoxiciliin, often is preferred because of its greater oral bioavailability and decreased gastrointestinal irritability]
Antimicrobials:

Although it works similarly to penicillins and cephalosporins, this monobactam is resistant to β-lactamases, and displays no cross-allergenicity with penicillins
Aztreonam

[Although it is ineffective against gram-positive or anaerobic bacteria, it works synergistically with aminoglycosides against gram-negative rods
Antimicrobials:

Inhibitor of bacterial cell wall synthesis, this agent is available as a topical preparation in many over-the-counter antibacterial ointments
Bacitracin

[This peptide antibiotic inhibits cell wall synthesis in gram-positive organisms; causes severe nephrotoxicity if used systemically]
Antimicrobials:

These extended-spectrum penicillins are particularly useful against infection with Pseudomonas and Enterobacter spp.
Carbenicillin
Piperacillin
Ticarcillin

[These agents can be used with penicillinase inhibitors and work synergistically with aminoglycosides]
Antimicrobials:

Used for the treatment of septic meningitis, because this cephalosporin has good penetration into the central nervous system
Ceftriaxone

[It demonstrates coverage against the leading causes of bacterial meningitis, including Streptococcus pneumoniae, Neisseria meningitidis, and Haemophilus influenzae; other third-generation cephalosporins such as cefixime, also are the drug of choice for treatment of Neisseria gonorrhoeae infection]
Antimicrobials:

Causes cyanosis and cardiovascular collapse in premature neonates deficient in hepatic gluconosyltransferase (gray baby syndrome)
Chloramphenicol

[A bacteriostatic inhibitor of protein synthesis, blocking peptidyl transferase activity at the 50S ribosome]
Antimicrobials:

Associated with myelosuppression, and rarely, an idiosyncratic, irreversible aplastic anemia
Chloramphenicol

[Because of its inhibition of red blood cell maturation, it is rarely used systemically; it is available as a topical preparation]
Antimicrobials:

Primary drug used for acute attacks and prophylaxis of malarial infection, although resistance is common
Chloroquine

[This drug kills parasites within erythrocytes [schizonticidal]; it disrupts hemoglobin breakdown, with the accumulation of heme, which is toxic to the organism]
Antimicrobials:

Administered with penicillins to enhance their antimicrobial effects
Clavulanic Acid
Sulbactam
Tazobactam

[Inhibit β-lactamases, resulting in increased microbial coverage]
Antimicrobials:

Antibiotic associated with the development of pseudomembranous colitis, due to overgrowth of Clostridium difficile
Clindamycin

[A bacteriostatic inhibitor of protein synthesis, methylating the 50S ribosomal subunit, used in the treatment of serious anaerobic infections due to Bacteroides spp.]
Antimicrobials:

Used in combined regimens for the treatment of HIV infection, this drug is associated with a dose-limiting pancreatitis
Didanosine (ddl)

[Other nucleoside reverse transcriptase inhibitors (NRTI) include zidovudine (ZDT), zalcitabine (ddC), lamivudine (3TC), and stavudine (d4T); lamivudine is unique in that it also inhibits the reverse transcriptase of hepatitis B virus]
Antimicrobials:

Side effects of this widely used antibiotic include gastrointestinal irritation and a hypersensitivity-based acute cholestatic hepatitis
Erythromycin

[Bacteriostatic inhibitor of protein synthesis, functioning on the 50S ribosome; erythromycin and the other macrolides, azithromycin and clarithromycin, show good coverage against Mycoplasma, Corynebacterium, Chlamydia, Legionella, and Bordetella spp.]
Antimicrobials:

Can cause tendon damage in adults, and is contraindicated in children and pregnant women because of damage to developing cartilage
Fluoroquinolones
(Ciprofloxacin/Norfloxacin)

[Bactericidal inhibitor of DNA gyrase, used for gram-negative rods, Neisseria spp., and some gram-positive organisims]
Antimicrobials:

Imidazole antifungal used for the treatment of fungal meningitis, because it can cross the blood-brain barrier
Fluconazole

[The drug inhibits the formation of ergosterol, and lacks the antiendocrine effects seen with ketoconazole. It is also used for prophylaxis against Cryptococcus neoformans, and it is effective in the treatment of esophageal and oropharyngeal candidiasis.]
Antimicrobials:

Back-up drug used for the treatment of cytomegalovirus infection in immunocompromised patients, when resistance to ganciclovir develops
Foscarnet

[The drug does not require phosphorylation by viral kinases and inhibits viral DNA polymerase at a different site than ganciclovir; it also is not metabolized by viral transferases, which render ganciclovir ineffective.]
Antimicrobials:

Used for the treatment of retinitis and other infections associated with cytomegalovirus (CMV)
Ganciclovir

[Guanosine analog converted by CMV to a triphosphorylated form which inhibits the viral polymerase; given IV, it has good penetration to the eye and CNS, but causes neutropenia, leukopenia, and thrombocytopenia]
Antimicrobials:

Given orally, this antifungal accumulates in keratinized tissue and is effective against dermatophyte infections, such as ringworm (tinea)
Griseofulvin

[The drug binds to tubulin, inferfering with microtubule function, thus inhibiting mitosis]
Antimicrobials:

Broad-spectrum β-lactamase-resistant carbapenem, administered in conjunction with cilastatin
Imipenem

[Used against gram-positive cocci, gram-negative rods, and anaerobes. It is metabolized by renal dihydropeptidase, which is blocked by the coadministration of cilastatin.]
Antimicrobials:

Protease inhibitors used in combined treatment regimens for HIV infection
Indinavir
Ritonavir
Saquinavir
Nelfinavir

[These agents inhibit the protease encoded by HIV pol gene and required for the production of infectious virions; these compounds are metabolized by the cytochrome P450 system]
Antimicrobials:

This agent is recommended for the prophylaxis of tuberculosis in skin test converters and in people who have close contact with patients with active disease. It is also the primary drug in most multidrug regimens for the treatment of active tuberculosis.
Isoniazid (INH)

[Inhibits the synthesis of mycolic acid in the mycobacterial cell wall; because it is acetylated by the liver, side effects include peripheral neuritis in slow acetylators and hepatitis in fast acetylators. Due to the emergence of multidrug- resistant strains of Mycobacterium tuberculosis, multidrug regimens also include ethambutol, pyrazinamide, rifampin, and streptomycin.]
Antimicrobials:

Antihelminthic agent used for the treatment of river blindness (caused by Onchocerca volvulus) and threadworm infection (Strongyloides stercoralis)
Ivermectin

[Increases GABA-mediated neurotransmission, but since it does not cross the human blood-brain barrier, it selectively affects the nematode, resulting in paralysis of the worm]
Antimicrobials:

Used for the treatment of mycotic infections, these agents inhibit hormone production and result in gynecomastia
Azoles
(Ketoconazole/Itraconazole/Fluconazole)

[These drugs interfere with fungal cell wall synthesis by inhibiting the 14α-demethylation of lanosterol; the demethylation is catalyzed by the cytochrome P450 system]
Antimicrobials:

Used for the treament of many helminth infections, it is the drug of choice for pinworms, the most common helminth infection in the United States
Mebendazole

[Functions by inhibiting microtubule synthesis and glucose uptake in helminths; related drugs such as albendazole and thiabendazole are alternatives]
Antimicrobials:

Narrow-spectrum, penicillinase-resistant β-lactam antibiotics, used to treat penicillin-resistant Staphylococcus aureus
Methicillin
Nafcillin
Dicloxacillin

[Bulkier R-groups on the penicillin backbone prevent degradation by penicillinases]
Antimicrobials:

Antiprotozoal agent used in the treatment of amebiasis, trichomoniasis, and giardiasis, as well as for pseudomembranous colitis
Metronidazole

[Undergoes activation by anaerobes and parasites to create products that interfere with nucleic acid synthesis, resulting in cytotoxicity]
Antimicrobials:

Aminoglycoside given orally for prophylaxis in bowel surgery, and also used to treat hepatic encephalopathy
Neomycin

[This drug prevents the growth of GI flora and the accumulation of nitrogenous microbial metabolites, which contribute to the development of hepatic encephalopathy; too toxic to be administered IV, but often used topically in over-the-counter antibiotic ointments]
Antimicrobials:

Nonnucleoside reverse-transcriptase inhibitors (NNRTIs) used in the management of HIV infection
Nevirapine
Delavirdine
Efavirenz

[Because these drugs bind to a unique site on reverse transcriptase, there is no cross-resistance with the nucleoside reverse-transcriptase (NRTIs); the NNRTIs are all metabolized by the P450 system]
Antimicrobials:

Trypanosomicidal drug used for the treatment of Chagas disease
Nifurtimox

[Drugs used to treat African trypanosomiasis include pentamidine, suramin, and melarsoprol]
Antimicrobials:

Urinary antiseptic that requires acidification and therefore is ineffective systemically, although toxic levels can accumulate with renal failure
Nitrofurantoin

[Can cause GI side effects, rash, hemolysis in glucose-6-phosphate dehydrogenase deficiency patients]
Antimicrobials:

"Swish and swallow" treatment for oral candidiasis, or topically for the treatment of diaper rash
Nystatin

[Disrupts fungal membrane permeability by binding to ergosterol]
Antimicrobials:

Orally active antiviral drug used to decrease the duration and symptoms of influenze A infection
Oseltamivir

[Zanamivir is a similar drug, but it is administered intranasally; both drugs function as neuroaminidase inhibitors, preventing the spread of virus from cell to cell]
Antimicrobials:

This group of bactericidal antibiotics inhibits the transpeptidation step during cell wall synthesis, resulting in the activation of autolytic enzymes, which destroy the bacteria
Penicillins

[The mechanism of cephalosporins is nearly identical; major side effects include hypersensitivity and urticaria, and rarely, anaphylaxis leading to life-threatening asphyxiation]
Antimicrobials:

This antibiotic disrupts bacterial membranes and is often too toxic to be administered systemically, although it is safe topically
Polymyxin B

[This agent acts as a cationic detergent that disrupts the membrane; systemic use causes neurotoxicity and acute tubular necrosis]
Antimicrobials:

Primary drug used for the treatment of trematode (fluke) and cestode (tapeworm) infections
Praziquantel

[Increases calcium permeability in the worm resulting in paralysis; niclosamide, which functions by uncoupling oxidative phosphorylation (inhibiting ATP production) or by activating ATPases, often is used with praziquantel in cestode infections]
Antimicrobials:

Antihelmenthic agent, often used with mebendazole for the treatment of roundworm, pinworm, and hookworm infections
Pyrantel Pamoate

[Stimulates nicotinic receptors in the nematode, resulting in a spastic paralysis]
Antimicrobials:

Used for the treatment of chloroquine-resistant malarial infection due to Plasmodium falciparum
Quinine

[Blocks DNA replication and RNA transcription in P. falciparum within erythrocytes; a common side effect is cinchonism, a constellation of symptoms including headache, vertigo, blurred vision, and tinnitus; a related drug, mefloquine, has fewer side effects and is used as prophylaxis in chloroquine-resistant areas]
Antimicrobials:

Administered as an aerosol, this drug is used for the treatment of respiratory syncytial virus (RSV) infection
Ribavirin

[Guanosine analog that inhibits formation, the capping of viral mRNA, and viral RNA-dependent RNA polymerase activity; also used for the management of viral hemorrhagic fevers and hepatitis C infection]
Antimicrobials:

Rarely used alone, except for the treatment of the meningococcal carrier state, this drug imparts a red-orange color to secretions
Rifampin

[Inhibits DNA-dependent RNA polymerase; often used in a combined drug regimen for Mycobacterium tuberculosis because of rapid resistance if used alone]
Antimicrobials:

This class of antibiotics that inhibits protein synthesis and is effective in the treatment of methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE)
Streptogramins

[Synercid is a mixture of quinupristin and dalfopristin; use has been associated with arthralgias and myalgias, as well as inhibition of P450 enzymes]
Antimicrobials:

Contraindicated in pregnant women and children, because it causes bone dysplasia and defects in dental enamel
Tetracycline

[Broad-spectrum bacteriostatic drug that inhibits the 30S ribosome and thus protein synthesis; provides good coverage against Mycoplasma, Chlamydia, Rickettsia, and Vibrio spp.]
Antimicrobials:

These two drugs create a block in successive reactions for folate synthesis; also often used to treat urinary tract infections
Trimethoprim and Sulfamethoxazole

[Trimethoprim blocks bacterial dihydrofolate reductase and can cause megaloblastic anemia; sulfamethoxazole blocks dihydropteroate synthase and can cause hypersensitivity reactions and hemolysis in patients with glucose-6-phosphate dehydrogenase (G6PD or G6PDH) deficiency]
Antimicrobials:

Rapid IV infusion is associated with diffuse flushing ("red man" syndrome)
Vancomycin

[Used for the treatment of methicillin-resistant Staphylococcus aureus (MRSA), and pseudomembranous colitis due to Clostridium difficile; side effects can be limited by infusion over a prolonged period and coadministration of antihistamines]
Antimicrobials:

Commonly used as part of highly active anti-viral therapy (HAART), this HIV drug is used for prophylaxis of needlestick transmission and of transmission to neonated from infected mothers during birth
Zidovudine (ZDV)

[Formerly known as AZT, phosphorylation of this agent by host cell enzymes results in inhibiting viral reverse transcriptase, as well as functioning as a chain terminator.
AZT slows HIV spread significantly, but does not stop it entirely. This allows HIV to become AZT resistant over time, and for this reason AZT is usually used in conjunction with other nucleoside reverse transcriptase inhibitors (NRTIs) and anti-viral drugs. In this form, AZT is used as an ingredient in Combivir and Trizivir, among others.]
Cancer:

Inhibits the enzyme aromatase and is used for the treatment of estrogen-dependent breast cancer
Anastrozole

[An inhibitor of steroid synthesis, it inhibits the conversion of androstenedione to estrone. Aminoglutethimide is a similar drug that inhibits the conversion of cholesterol to pregnenolone, and is used for the same types of cancers]
Cancer:

This antineoplastic agent is used for the treatment of testicular carcinoma and squamous cell carcinoma; it can cause life-threatening pulmonary fibrosis
Bleomycin

[The drug is a mixture of glycoproteins that results in the production of free radicals after binding to DNA, creating single-and double-stranded breaks. This G2 phase inhibitor is a part of the ABVD regimen (adriamycin, bleomycin, vinblastine, and dacarbazine) for Hodgkin's disease]
Cancer:

Highly lipophilic nitrosureas that readily cross the blood-brain barrier and are used for the treatment of many brain tumors
Carmustine (BCNU)
Lomustine (CCNU)

[These alkylating agents result in DNA cross-linking and strand breaks]
Cancer:

Platinum-containing compound used in the treatment of testicular and lung cancers
Cisplatin

[Acts as an alkylating agent and causes nephrotoxicity and acoustic nerve damage; a similar agent, carboplatin, has less nephrotoxicity and neurotoxicity, but greater myelosuppression]
Cancer:

Alkylating agent used for the treatment of non-Hodgkin's lymphoma and breast and ovarian carcinomas
Cyclophosphamide

[The major side effect, hemorrhagic cystitis, may be decreased by vigorous hydration and the use of mesna]
Cancer:

Part of the AVDB regimen, an antibiotic-type compound used in the treatment of myelomas, sarcomas, and lymphomas
Doxorubicin (Adriamycin)

[Intercalates in DNA to decrease replication and transcription; this drug is associated with significant cardiotoxicity and dilated cardiomyopathy. Daunorubicin is a similar drug and is used primarily for the treatment of acute myelogenous leukemia (AML) and acute lymphocytic leukemia (ALL).]
Cancer:

Inhibitor of topoisomerase II used for the treatment of small cell carcinoma of the lung and prostate, and testicular cancers
Etoposide

[G2 phase-specific inhibition, resulting in double-stranded DNA breaks and degradation]
Cancer:

Inhibits thymidylate synthase, resulting in thymineless death, and is used for the treatment of colon cancer and superficial tumors, such as basal cell carcinoma
Fluorouracil (5-U)

[This S-phase antimetabolite causes myelosuppression]
Cancer:

Androgen receptor antagonist, used for the treatment of carcinoma of the prostate
Flutamide

[Used to antagonize residual androgens after orchiectomy; side effects include gynecomastia and libido changes]
Cancer:

Recombinantly produced cytokine, used for the hairy cell leukemia
Interferon Alpha

[Also used for the treatment of chronic myelogenous leukemia (CML), malignant melanoma, and Kaposi's sarcoma; it normally is produced by virally infected cells to prevent infection of adjacent cells]
Cancer:

Gonadotropin-releasing hormone (GnRH) agonists, used for the treatment of metastatic carcinoma of the prostate
Leuprolide
Goserelin
Nafarelin

[May be used for the treatment of endometriosis, benign prostatic hyperplasia, and precocious puberty; if administered in a pulsatile manner, they stimulate the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), and can thus be used in the management of infertility]
Cancer:

Purine metabilites, used for the treatment of leukemias and lymphomas
Mercaptopurine (6-MP)
Thioguanine (6-TG)

[Requires activation by hypoxanthine-guanine phosphoribosyltransferase (HGPRT), and inhibits many enzymes involved in purine metabolism]
Cancer:

Folic acid analog, used for the treatment of leukemias, non-Hodgkin's lymphoma, rheumatoid arthritis, and therapeutic abortions
Methotrexate

[S phase inhibitor of dihydrofolate reductase, leading to decreased DNA and protein synthesis; the accompanying myelosuppression can be treated with leucovorin]
Cancer:

Microtubule stabilizing agent, used for the treatment of lung, ovarian, breast cancer, head and neck cancer, and advanced forms of Kaposi's sarcoma
Paclitaxel

[Derived from the yew tree, this M phase agent prevents the mitotic spindle from breaking down and thus inhibits completion of anaphase]
Cancer:

Glucocorticoid used for the treatment of leukemias and lymphomas, as well as for rheumatoid arthritis and asthma
Prednisone

[Triggers apoptosis and can lead to hypercortisolism with Cushing-like symptoms. Drug must be tapered gradually to prevent life-threatening adrenal insufficiency.]
Cancer:

Monoclonal antibody used for the treatment of low-grade non-Hodgkin's lymphoma
Rituximab

[Binds to the CD20 antigen on B cells; adverse reactions are associated with infusion, and include fever, chills, headache, and nausea]
Cancer:

Primary agent used in the treatment of estrogen receptor-positive breast cancer
Tamoxifen

[An estrogen receptor partial agonist, which may increase the risk of endometrial carcinoma]
Cancer:

Monoclonal antibody used for the treatment of metastatic breast cancer
Trastuzumab

[Binds to the receptor tyrosine kinase Erb-B2 (HER-2), overexpressed on some breast cancers)
Cancer:

Vinca alkaloid used as part of the MOPP regimen for lymphomas, Wilms tumor, and choriocarcinomas
Vincristine (Oncovin)

[M phase inhibitor that blocks microtubule polymerization and spindle formation; a similar agent, vinblastine, is part of the ABVD regimen. The ABVD regimen includes the combined used of adriamycin, bleomycin, vinblastine, and dacarbazine whereas the MOPP regimen includes the use of mechlorethamine, Oncovin (vincristine), procarbazine, and prednizone.]
Toxicology:

Used to treat the ingestion of suicidal doses of acetaminophen
N-Acetylcysteine

[Given early, it may protect from the development of fulminant hepatic failure]
Toxicology:

Antispasmodic used for the treatment of malignant hyperthermia and neurologic malignant syndrome
Dantrolene

[Decreases the release of calcium from the sarcoplasmic reticulum]
Toxicology:

Used for the treatment of acute iron toxicity
Deferoxamine

[Rapid infusion has been associated with hypotensive shock]
Toxicology:

Fab fragment antibody used for the treatment of digitalis toxicity
Digibind

[Treatment also includes the correction of Mg⁺2 and K⁺, as well as lidocaine for induced arrhythmias]
Toxicology:

Agent used to treat heavy metal poisoning due to lead, arsenic, and mercury
Dimercaprol

[Given parenterally, it chelates metals, preventing them from damaging proteins; succimer is an orally available derivative used for similar applications]
Toxicology:

Ingestion, industrial inhalation, or absorption through the skin causes metabolic acidosis and the precipitation of damaging oxalate crystals in the kidney
Ethylene Glycol

[A major component of antifreeze, toxicity is managed by the administration of ethanol]
Toxicology:

Used in the event of benzodiazepine overdose
Flumazenil

[This benzodiazepine derivative antagonizes the actions of benzodiazepines and zolpidem, although it does not block the actions of barbiturates]
Toxicology:

Intoxicant that can cause retinal damage and blindness along with metabolic acidosis and coma
Methanol

[Damage is due to the conversion to formaldehyde by the liver; the treatment includes ethanol, which competes for alcohol dehydrogenase]
Toxicology:

Used to treat the symptoms of opioid overdose
Naltrexone
Naloxone

[Pure antagonists, primarily of mu opioid receptors]
Toxicology:

Anticholinesterases used as insecticides and as possible agents of chemical warfare, inducing motor paralysis, respiratory depression, and convulsions
Organophosphates
(Isoflurophate/Echothiophate/Parathion)

[Antidote includes the use of atropine and acetylcholinesterase regenerators, such as pralidoxime]
Toxicology:

Derivative of penicillin with the ability to chelate copper ions, used for the treatment of copper toxicity
Penicillamine

[Also used for the treatment of Wilson's disease, and an adjunct therapy for rheumatoid arthritis]
Shared Effects:

Drugs that cause significant ototoxicity and nephrotoxicity
Aminoglycosides (antibiotics)
Loop Diuretics
Cisplatin (Antineoplastic)

[Vancomycin rarely is associated with mild ototoxicity and nephrotoxicity, although both may become significant when used in conjunction with aminoglycosides]
Shared Effects:

Drugs that lead to pulmonary fibrosis and subsequent restrictive lung disease
Bleomycin (Antineoplastic)
Amiodarone (Class IA Antiarrhythmic)
Busulfan (Antineoplastic)

[Patients may manifest with dyspnea, tachypnea, and eventual cyanosis, with a decreased forced expiratory volume at 1 second (FEV₁) and a decreased forced vital capacity (FVC)]
Shared Effects:

Drugs that cause gynecomastia
Cimetidine (Antiulcer)
Ketoconazole (Antifungal)
Spironolactone (Antihypertensive)

[All compete for androgen receptors, leading to antiandrogenic effects]
Shared Effects:

Common drugs that inhibit hepatic P450 system
Cimetidine (Antiulcer)
Ketoconazole (Antifungal)
Erythromycin (Antibiotic)

[Such drugs potentiate the action of other drugs which are normally metabolized by the P450; often doses must be lowered when such drugs are used together]
Shared Effects:

Drugs that can cause massive hepatic necrosis
Halothane (Anesthetic)
Acetaminophen (Analgesic)
Valproic Acid (Anticonvulsant)

[Histologically, damage to the liver is indistinguishable from that chronic viral hepatitis]
Shared effects:

Drugs that cause a systemic lupus erythematosus (SLE)-like syndrome
Hydralazine (Vasodilator)
Procainamide (Class IA Antiarrhythmic)
Isoniazid (Antituberculoid)
Phenytoin (Anticonvulsant)

[Symptoms include arthralgias, myalgias, skin rashes, and fever]
Shared effects:

Drugs that inhibit microtubule function
Mebendazole (Antihelminthic)
Thiabendazole (Antihelminthic)
Paclitaxel (Antineoplastic)
Vincristine (Antineoplastic)
Colchicine (Antigout)
Griseofulvin (Antifungal)

[These agents either block intracellular transport, interfere with locomotion, or disrupt the formation of the mitotic spindle]
Shared effects:

Drugs that cause a disulfram-like reaction
Metronidazole (Antibiotic)
Certain cephalosporins (Antibiotic)
Procarbazine (Antineoplastic)

[Cause flushing, headache, nausea, sweats, hypotension, and confusion]
Shared effects:

Drugs that cause cutaneous flushing on administration
Niacin (Antihyperlipidemic)
Calcium Channel Blockers
Adenosine (Antiarrhythmic)
Vancomycin (Antibiotic)

[Often this side effect can be controlled by slow infusion or coadministration with histamine blockers]
Shared effects:

Bactericidal antibiotics
Penicillins
Cephalosporins
Vancomycin
Aminoglycosides
Fluoroquinolones
Metronidazole

[Most of the other antibiotics are bacteriostatic]
Shared effects:

Drugs that induce the hepatic P450 system
Phenytoin (Anticonvulsant)
Carbamazepine (Anticonvulsant)
Griseofulvin (Antifungal)
Rifampin (Antituberculoid)
Barbiturates
Chronic Ethanol Use

[The hepatic P450 microsomal mixed function oxidase system is involved in phase I metabolism of many drugs]
Shared effects:

Drugs that cause a Stevens-Johnson syndrome, a febrile, erosive hemorrhagic crusting on the lips and oral mucosa of children
Sulfonamides (Antibiotic)
Ethosuximide (Anticonvulsant)
Lamotrigine (Anticonvulsant)

[Other agents such as penicillins, barbiturates, salicylates, hydantoins, and antimalarials may be associated with a less severe form of erythema multiforme, with macules, papules, vesicles, and bullae]
Shared effects:

Drugs that can cause hemolysis in patients with glucose-6 phosphate dehydrogenase (G6PD) deficiency
Sulfonamides (Antibiotic)
Isoniazid (Antituberculoid)
Primaquine (Antimalarial)

[In patients with G6PD deficiency, these agents cause oxidative stress on RBCs because of a deficit of reducing equivalents of nicotinamide adenine dinucleotide phosphate (NADPH), normally generated by the hexose monophosphate shunt]
Shared effects:

Drugs that cause photosensitivity
Tetracycline (Antibiotic)
Amiodarone (Class IA Antiarrhythmic)
Sulfonamides (Antibiotics)

[Barbituates can precipitate photosensitivity in patients with acute intermittent porphyria]