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BRS Pharm Flashcards

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USMLE® Step 1 flashcards
1
Q

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

A

ATROPINE
▸ The side effects for 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”.

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2
Q

Muscarinic Agonist used to treat postoperative urinary retention and atonic ileus

A

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

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3
Q

Short–acting anticholinesterase used to confirm the diagnosis of myasthenia gravis

A

EDROPHONIUM

▸ IV injection of this rapidly absorbed drug results in an appreciable increase in muscle strength

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4
Q

Indirect–acting sympathomimetic used in OTC nasal decongestants

A

EPHEDRINE
▸ It has many of the same actions as amphetamines, with less CNS stimulation
▸ It is found in Chinese herbs such as ma–huang
▸ One enantiomer, Pseudoephedrine, is found in many cold–relief medications

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5
Q

Adrenergic Agonist used for acute asthma, anaphylactic shock, open–angle glaucoma, and cardiac resuscitation

A

EPINEPHRINE
▸ Adrenergic Agonist with affinity for alpha–1, alpha–2, beta–1, and beta–2 receptors.
▸ At low concentrations the effects of the beta receptors predominate. Beta–2 receptors cause vasodilation with decreased total peripheral resistance (TPR) and decreased diastolic pressure.
▸ At higher concentrations, beta–1 receptors lead to increase cardiac contractility and increased heart rate

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6
Q

Prototypic Beta Agonist used for the treatment of both acute heart failure and acute asthma

A

ISOPROTERENOL
▸ This agent has equivalent affinities for beta–1 and beta–2 receptors
▸ The beta–1 activity causes an increase in cardiac contractility and increased heart rate, resulting in increased stroke volume and cardiac output
▸ The beta–2 activity induces bronchodilation

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7
Q

Adrenergic Antagonist used in the treatment of benign prostatic hyperplasia and in the management of hypertension caused by pheochromocytoma

A

PHENOXYBENZAMINE
▸ An irreversible alpha–1 and alpha–2 antagonist
▸ A similar short–acting reversible antagonist, Phentolamine, is used in the diagnosis of pheochromocytoma

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8
Q

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

A

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

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9
Q

▸ Used to treat hypertension and urinary retention

▸ First–dose syncope is a significant side effect associated with this drug

A

PRAZOSIN
▸ A competitive alpha–1 antagonist
▸ The use of this drug can lead to postural hypotension, inhibition of ejaculation, reflex tachycardia, nasal congestion, and miosis

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10
Q

Prototypical Beta Antagonist used in the treatment of:
▸ Hypertension, glaucoma, migraines, and angina
▸ As a prophylaxis for myocardial infarctions
▸ At low doses to prevent performance anxiety

A

PROPRANOLOL
▸ Nonselective beta–1 and beta–2 blocker
▸ Not to be used in patients with COPD and asthma, due to significant bronchoconstriction

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11
Q

Long–acting anticholinesterase used in the chronic treatment of myasthenia gravis

A

PYRIDOSTIGMINE
▸ Also used as an antidote to Tubocurarine toxicity
▸ Neostigmine is a similar substance, although is has a shorter duration of action

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12
Q

Used to prevent motion sickness and delivered by a transdermal patch

A

SCOPOLAMINE

▸ Competitive cholinergic antagonist with sedating and amnestic effects

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13
Q

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

A

SUCCINYLCHOLINE
▸ Functions as a cholinergic nicotinic agonist, facilitating the opening of sodium channels
▸ A rare but significant side effect, malignant hyperthermia, can occur in some patients when used with Halothane

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14
Q

Nondepolarizing neuromuscular ganglionic blockers used in surgical anesthesia (3)

A

TUBOCURARINE, PANCURONIUM, MIVACURIUM
▸ 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

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15
Q

▸ Diuretic used in the management of chronic glaucoma and acute mountain sickness
▸ Also used to alkalinize the urine in aspirin toxicity

A

ACETAZOLAMIDE
▸ Inhibits carbonic anhydrase in the proximal convoluted tubule
▸ Metabolic acidosis is a potential side effect

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16
Q

Potassium–sparing diuretics that do not have anti–androgenic effects (2)

A

AMILORIDE, TRIAMTERENE
▸ Block sodium channels in the cortical collecting tubules
▸ May cause hyperkalemic metabolic acidosis

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17
Q

Cough is a major side effect of this group of antihypertensive drugs

A 
ACE INHIBITORS (CAPTOPRIL, ENALAPRIL, LISINOPRIL)
▸ Inhibit the conversion of Angiotensin I to Angiotensin II
▸ Inhibit breakdown of Bradykinin, resulting in cough and potent vasodilation
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18
Q

Most potent class of diuretics that inhibit the Na+/K+/Cl– cotransporter in the thick ascending loop of Henle

A

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

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19
Q

Diuretic that functions early in the distal convoluted tubule by inhibiting NaCl reabsorption

A

HYDROCHLOROTHIAZIDE

▸ Major side effects include hypokalemia, alkylosis, hyperuricemia, & hyperlipidemia

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20
Q

Angiotensin II Receptor Antagonist used as an antihypertensive drug

A

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 in pregnancy

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21
Q

▸ Osmotic diuretic that works by extracting water from tissues into the blood
▸ Used in the Tx of hydrocephalus and increased intracranial pressure

A

MANNITOL
▸ This diuretic fxns primarily WITHIN THE PCT’s and is used to maintain HIGH URINE OUTPUT in cases of severe HEMOLYSIS or RHABDOMYOLYSIS

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22
Q

Originally developed as an antihypertensive agent, it is used topically because of the beneficial side effect of hypertrichosis (growth of hair in excess of normal)

A

MINOXIDIL

▸ Fxns as a direct–acting vasodilator, as do NITROPRUSSIDE and HYDRALAZINE

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23
Q

This potent vasodilator, used in the Tx of malignant hypertension, can cause significant postural hypotension

A

NITROPRUSSIDE
▸ Fxns to STIMULATE GUANYLYL CYCLASE with an INCREASE IN cGMP within smooth muscle of the vasculature
▸ Prolonged infusion can result in CYANIDE POISONING due to RELEASE OF CN–

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24
Q

This Potassium–Sparing Diuretic is an Aldosterone Antagonist that fxns at the collecting tubule

A

SPIRONOLACTONE

▸ Increases P450 activity and causes GYNECOMASTIA and other ANTI–ANDROGENIC EFFECTS

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25
Q

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

A

ADENOSINE

▸ The side effects of FLUSHING AND HYPOTENSION are short–lived as well, and do not limit the use of this agent

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26
Q

Long–acting Class III anti–arrhythmic associated w/ pulmonary fibrosis, thyroid dysfunction, and corneal microdeposits

A

AMIODARONE

▸ This agent also blocks SODIUM CHANNELS, such as the CLASS IA anti–arrhythmics

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27
Q

Used for the Tx of CHF, this agent contains 2 isomers, one with nonselective beta blocking activity and one with alpha–1 blocking activity

A

CARVEDILOL
▸ LABETALOL has similar properties and has 4 diastereomers
▸ The RR enantiomer is a NONSELECTIVE BETA BLOCKER, and the SR enantiomer is an ALPHA–1 BLOCKER

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28
Q

Bile Acid–Binding Resins used in the mgmt of hyperlipidemia (2)

A

CHOLESTYRAMINE, COLESTIPOL
▸ BIND BILE ACIDS, PREVENTING ENTEROHEPATIC RECYCLING, thus diverting hepatic efforts to renew bile acids, INSTEAD OF PRODUCING PLASMA LIPIDS

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29
Q

These agents fxn to slow conduction velocity by slowing the rate and rise of the action potential

A

CLASS IA ANIT–ARRHYTHMICS (QUINIDINE, PROCAINAMIDE, DISOPYRAMIDE)
▸ These agents help MAINTAIN SA RHYTHM AFTER CARDIOVERSION FOR ATRIAL FIBRILLATION, and may cause TORSADE DE POINTES arrhythmias
▸ QUINIDINE may cause CINCHONISM, a type of poisoning that causes headache, vertigo, and tinnitus

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30
Q

Fxn to decrease the action potential duration by shortening the repolarization phase

A

CLASS IB ANTI–ARRHYTHMICS (LIDOCAINE, MEXILETINE, TOCAINIDE, PHENYTOIN)
▸ These agents are used for the Tx of VENTRICULAR ARRHYTHMIAS, as well as for DIGITOXIN–INDUCED ARRHYTHMIAS

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31
Q

Used for Tx of refractory ventricular arrhythmias, as well as for rapid atrial arrhythmias associated with Wolff–Parkinson–White Syndrome

A

CLASS IC ANTI–ARRHYTHMICS (FLECAINIDE, PROPAFENONE)
▸ Fxn to SLOW CONDUCTION VELOCITY in the atrial and ventricular cells but DO NOT AFFECT THE AP
▸ They typically are used as a LAST RESORT, as their use is associated with DRUG–INDUCED ARRHYTHMIAS.

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32
Q

These agents decrease the automaticity of the pacemaker tissue of the heart, resulting in prolonged AV conduction and slower HR

A

CLASS II ANTI–ARRHYTHMICS (PROPRANOLOL, ESMOLOL)
▸ These beta blockers DECREASE cAMP levels, resulting in REDUCED SODIUM AND CALCIUM CURRENTS
▸ These agents are NOT to be used in cases of CHF

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33
Q

▸ Used for the Tx of recurrent ventricular arrhythmias

▸ Many of these agents can precipitate torsade de pointe arrhythmias

A

CLASS III ANTI–ARRHYTHMICS (SOLATOL, IBUTULIDE, BRETYLIUM, AMIODARONE)
▸ These agents prolong the action potential by BLOCKING POTASSIUM CHANNELS

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34
Q

▸ Used for atrial arrhythmias and nodal re–entry, as well as hypertension and angina
▸ These agents inhibit Ca2+ voltage channels

A 
CLASS IV ANTI–ARRHYTHMICS (VERAPAMIL, DILTIAZEM)
▸ 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
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35
Q

Centrally–acting Alpha–2 Agonist that reduces sympathetic ANS outflow, resulting in decreased blood pressure

A

CLONIDINE

▸ A major side effect of this drug is REBOUND HYPERTENSION, in the event of ABRUPT DISCONTINUATION

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36
Q

Used in the mgmt of CHF, these drugs are reversible inhibitors of Na/K ATPase

A

DIGITOXIN, DIGOXIN
▸ Unlike Digitoxin, DIGOXIN IS SHORTER–ACTING and EXCRETED BY THE KIDNEYS
▸ Pts w/ LOW K+, LOW Mg, HIGH Na+, or high Ca2+ can EXPERIENCE ARRHYTHMIAS w/ either agent

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37
Q

Agents that decrease triglycerides dramatically by stimulating lipoprotein lipase

A

GEMFIBROZIL, FENOFIBRATE, CLOFIBRATE

▸ CLOFIBRATE has been associated with GALLSTONES and HEPATOBILIARY NEOPLASMS

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38
Q

Antihypertensives drug that blocks the release or norepinephrine by displacing it from intracellular vesicles

A

GUANETHIDINE
▸ Side effects include serious ORTHOSTATIC HYPOTENSION
▸ The effects of the drug are ANTAGONIZED BY TRICYCLIC ANTIDEPRESSANTS

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39
Q

Used for the Tx of ventricular arrhythmias, especially following MI, because it works only on ischemic tissue

A

LIDOCAINE
▸ This Class IB Anti–arrhythmic has LITTLE EFFECT on the ECG of NORMAL [NON–ISCHEMIC] HEART tissue
▸ It is given IV, although similar agents [MEXILETINE and TOCAINIDE] are given orally

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40
Q

This Alpha–2 Agonist decreases adrenergic outflow from the CNS, resulting in decreased peripheral resistance and decreased blood pressure

A

METHYLDOPA

▸ This drug can haptenate RBC proteins, resulting in an AUTOIMMUNE HEMOLYTIC ANEMIA

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41
Q

Lipid–lowering agent that causes cutaneous flushing, which can be avoided by administering concurrently w/ Aspirin

A

NIACIN

▸ Directly REDUCES THE SECRETION OF VLDLs and apolipoprotein synthesis by the liver, while INCREASING HDLs

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42
Q

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

A

NITROGLYCERIN
▸ Administered as a SUBLINGUAL PATCH to DECREASE FIRST–PASS METABOLISM
▸ Potential side effects include CYANIDE POISONING, POSTURAL HYPOTENSION, HEADACHE, AND FLUSHING

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43
Q

Anti–hyperlipidemic Agent that may prevent atherosclerosis by acting as an antioxidant

A

PROBUCOL
▸ Rarely used for the Tx of hyperlipidemia because it DECREASES HDLs AS WELL AS LDLs
▸ May be efficacious in PREVENTING RE–STENOSIS after angioplasty

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44
Q

This rarely used anti–hypertensive agent blocks the storage and release of catecholamines and serotonin from neurons

A

RESERPINE

▸ The drug readily ENTERS THE CNS and can cause SUICIDAL DEPRESSION and PARKINSONIAN SYMPTOMS

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45
Q

Inhibits the rate–limiting enzyme of cholesterol synthesis, HMG–CoA Reductase, resulting in dramatically decreased LDL levels

A

STATINS (LOVASTATIN, PRAVASTATIN, SIMVASTATIN, ATORVASTATIN)
▸ May cause ELEVATED LIVER ENZYMES, MYOSITIS with INCREASED CREATINE KINASE from skeletal muscle, and, rarely, RHABDOMYOLYSIS

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46
Q

Intermediate–acting Benzodiazepine used for the Tx of panic disorder and phobias

A

ALPRAZOLAM
▸ Both ALPRAZOLAM and CLONAZEPAM have SEDATIVE effects and can cause physiologic DEPENDENCE
▸ BUSPIRONE is an alternative drug that binds 5–HT(1A) RECEPTORS w/ MINIMAL ABUSE POTENTIAL

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47
Q

Used in the mgmt of depression, it inhibits the re–absorption of both Norepinephrine and Serotonin within the synapse

A

AMITRIPTYLINE
▸ Other TRICYCLIC ANTIDEPRESSANTS include NORTRIPTYLINE, IMIPRAMINE and DESIPRAMINE
▸ Major side effects of this class include SEDATION, ORTHOSTATIC HYPOTENSION, and CARDIAC ARRHYTHMIAS

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48
Q

Orally active anti–spasmodic agent

A

BACLOFEN

▸ GABA–B RECEPTOR AGONIST that functions on inhibitory pathways in the spinal cord

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49
Q

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

A

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

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50
Q

This anti–muscarinic is used in the mgmt of Parkinson disease, improving tremors and rigidity, but does little for bradykinesia

A

BENZTROPINE
▸ As for all ANTI–MUSCARINICS, contraindications include PROSTATIC HYPERPLASIA, GI OBSTRUCTION, and closed–angle GLAUCOMA, which are more common in older Pts

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51
Q

Drug used in the Tx of Parkinson Disease as well as in the Tx of Prolactinoma

A

BROMOCRIPTINE
▸ This ergot derivative acts as a D2 AGONIST, improving extrapyramidal fxn, and also INHIBITS THE RELEASE OF PROLACTIN from the pituitary gland
▸ Unlike a similar agent, PERGOLIDE, Bromocriptine maintains its effectiveness over time

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52
Q

This long–acting amide–type local anesthetic can cause severe hypotension and arrhythmias if inadvertently given IV

A

BUPIVICAINE
▸ Local anesthetics BIND TO SODIUM CHANNELS in the OPEN AND INACTIVE STATE, SLOWING RECOVERY from depolarization 10– to 1000–fold

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53
Q

Antidepressant used in the mgmt of nicotine withdrawal in pts seeking to stop cigarette smoking with minimal sedation

A

BUPROPRION
▸ This second–generation HETEROCYCLIC ANTIDEPRESSANT inhibits the REUPTAKE OF NOREPI
▸ Newer third–generation agents used for depression, such as VENLAFAXINE, inhibit the reuptake of SEROTONIN as well

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54
Q

This agent is used in the Tx of partial and generalized seizures, and is the primary agent used in the Tx of neuralgia

A

CARBAMAZEPINE
▸ INHIBITS SODIUM CHANNELS on neurons
▸ Its use may result in IDIOSYNCRATIC BLOOD DISORDERS such as APLASTIC ANEMIA and AGRANULOCYTOSIS

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55
Q

Second–line Tx for schizophrenia that is better for the negative symptoms of the disease

A

CLOZAPINE
▸ ATYPICAL ANTIPSYCHOTIC, associated with AGRANULOCYTOSIS
▸ Blocks the D4 RECEPTOR

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56
Q

The only local anesthetic with vasoconstrictor activity

A

COCAINE

▸ OTHER local anesthetics are ADMINISTERED WITH EPI to increase the duration of action and LOWER THE EFFECTIVE DOSE

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57
Q

▸ Used for Tx of anxiety and ethanol dependence

▸ Also a primary agent in the Tx of status epilipticus

A

DIAZEPAM
▸ This long–acting, prototypic BENZODIAZEPINE binds to the GABA–A RECEPTOR, increasing the FREQUENCY OF CHLORIDE CHANNEL OPENING

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58
Q

Used in the Tx of Parkinson Disease, it inhibits the enzyme catechol–O–methyltransferase (COMT)

A

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

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59
Q

Preferred agent in the Tx of absence seizures

A

ETHOSUXAMIDE
▸ Postulated to fxn by INHIBITING T–TYPE CALCIUM CHANNELS in thalamic neurons
▸ Use has been associated with the development of STEVENS–JOHNSON SYNDROME

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60
Q

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

A

FENTANYL
▸ If used in conjunction with DROPERIDOL and NITROUS OXIDE, it can produce a state of NEUROLEPTANESTHESIA, resulting in both ANALGESIA AND AMNESIA

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61
Q

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

A

FLUOXETINE
▸ Common side effects of this and other SSRIs, such as SERTRALINE, PAROXETINE, AND CITALOPRAM, include headache, INSOMNIA, nausea, and SEXUAL DYSFUNCTION
▸ These agents also are used in the mgmt of OBSESSIVE COMPULSIVE DISORDER [OCD], SOCIAL PHOBIAS, bulimia, and alcohol dependence

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62
Q

This analog of GABA used in the Tx of partial seizures, as well as in the mgmt of peripheral neuropathy

A

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

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63
Q

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

A

HALOTHANE

▸ Rare but significant side effects include the development of MALIGNANT HYPERTHERMIA and FULMINANT HEPATITIS

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64
Q

Dissociative anesthetic that causes hallucinations and disorientation on recovery

A

KETAMINE

▸ Side effects are due to an INCREASE IN CEREBRAL BLOOD FLOW, and can be reduced by preoperative use of benzodiazepines

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65
Q

Used in the Tx of Parkinson Disease, this precursor crosses the BBB and is converted to dopamine

A

L–DOPA (LEVODOPA)
▸ Administered with the DECARBOXYLASE INHIBITOR, CARBIDOPA [which does not cross the BBB], to increase bioavailability and to LIMIT PERIPHERAL SIDE EFFECTS

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66
Q

Mood stabilizer that is a first–line drug for the Tx of bipolar affective disorder

A

LITHIUM
▸ INHIBITS the secondary messengers Inositol Triphosphate [IP3] and Diacylglycerol [DAG] and causes TREMOR, HYPOTHYROIDISM, POLYDIPSIA, AND POLYURIA

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67
Q

Amphetamine used in the mgmt of Attention Deficit Disorder (ADD) and Narcolepsy

A

METHYLPHENIDATE
▸ INCREASES ALERTNESS and DECREASES APPETITE by stimulating the RELEASE OF CATECHOLAMINES
▸ It is a controlled substance with ABUSE POTENTIAL

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68
Q

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

A

NITROUS OXIDE
▸ This gas has a HIGH MINIMAL ALVEOLAR CONCENTRATION [MAC] and a low blood/gas partition
▸ It usually is ADMINISTERED WITH AN IV ANESTHETIC such as THIOPENTAL, and is commonly used in DENTAL PROCEDURES

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69
Q

This older agent used in the Tx of depression increases levels of amine neurotransmitters by inhibiting their breakdown

A

MONOAMINE OXIDASE INHIBITORS (MAOIs) [PHENELZINE, TRANYLCYPROMINE, 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 SSRIs, life–threatening SEROTONIN SYNDROME can result

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70
Q

▸ Used as a sedative
▸ First line drug for tonic–clonic seizures in children
▸ Tx of Crigler–Najjar Syndrome Type II

A

PHENOBARBITAL
▸ As a long–acting, prototypical BARBITURATE, it binds to GABA RECEPTORS, increasing the DURATION OF CHLORIDE CHANNEL OPENING with neuronal INHIBITION

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71
Q

▸ Drug used for the Tx of Partial and Tonic–Clonic Seizures and Status Epilipticus
▸ Class IB Anti–Arrhythmic

A

PHENYTOIN
▸ Side effects include GINGIVAL HYPERPLASIA, HIRSUTISM, ANEMIA, AND BIRTH DEFECTS, because it INTERFERES WITH FOLATE ABSORPTION

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72
Q

This agent has the largest number of extrapyramidal side effects of all the Atypical Antipsychotics

A

RISPERIDONE
▸ ATYPICAL ANTIPSYCHOTICS block the D2 and 5–HT2 RECEPTORS, contributing to HIGH SEDATION
▸ More Recently introduced agents such as OLANZAPINE have NO EXTRAPYRAMIDAL SIDE EFFECTS

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73
Q

Newly available agent used in the Tx of Parkinson Disease that forestalls the use of Levodopa

A

ROPINIROLE
▸ This agent has a lower incidence of postural hypotension, dyskinesia, vomiting, and hallucination, unlike most dopamine agonists
▸ It is NOT AN ERGOT DERIVATIVE
▸ A similar agent, PRAMIPEXOLE, also used

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74
Q

Inhibits the degradation of dopamine in the CNS and is used as an adjuvant to Levodopa in the Tx of Parkinson Disease

A

SELEGILINE

▸ Inhibits MAO–B, which selectively degrades DOPAMINE

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75
Q

Ultra–short–acting barbiturate used IV for the induction of surgical anesthesia

A

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

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76
Q

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

A

THIORIDAZINE
▸ This LOW–POTENCY Antipsychotic BLOCKS MOST DOPAMINE RECEPTORS in the CNS, and can cause postural hypotension, sedation, and CNS depression

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77
Q

Used in the Tx of most forms of Epilepsy, including Generalized Tonic–Clonic, Partial Absence, and Myoclonic Seizures, and in the Tx of Bipolar Disorder

A

VALPROIC ACID

▸ This agent has been associated with the development of NEURAL TUBE DEFECTS when administered to PREGNANT WOMEN

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78
Q

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

A

ZOLPIDEM
▸ Fxns 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

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79
Q

Causes feelings of euphoria and self–confidence, and, at chronic high doses, delusions and paranoia?

A

AMPHETAMINES

▸ Function as an indirect sympathomimetic by releasing stored catecholamines

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80
Q

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

A

COCAINE

▸ Inhibits catecholamine re–uptake, resulting in cardiotoxicity and hypertensive episodes

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81
Q

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

A

DISULFIRAM
▸ Inhibits Aldehyde Dehydrogenase, resulting in toxic accumulation of Acetaldehyde
▸ Drugs with similar side effects are said to have disulfiram–like reactions

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82
Q

Used in the management of Opioid Withdrawal and maintenance programs for addicts

A

METHADONE
▸ Used to treat nausea, chills, sweats, lacrimation, cramps, rhinorrhea, yawning, piloerection, diarrhea and tremor due to opiod withdrawal

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83
Q

Overdose causes constricted pupils, clammy skin, nausea, drowsiness, and respiratory depression with possible coma and death

A

OPIOIDS (HEROIN, MORPHINE, MEPERIDINE, FENTANYL)

▸ Modulate synaptic transmission by binding mu (morphine), delta (enkephalin), and kappa (dynorphin) receptors

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84
Q

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

A

ACETAMINOPHEN
▸ Weak COX inhibitor, it inhibits Prostaglandin synthesis in the CNS
▸ A related prodrug, Phenacetin, is no longer available due to nephrotoxicity

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85
Q

Used in the management of Chronic Gout and as an adjunct to cancer chemotherapy, to slow the production of uric acid

A

ALLOPURINOL
▸ Results in suicide inhibition of Xanthine Oxidase with the resultant increase of Xanthine and Hypoxanthine, both of which are more soluable and less likely to form crystals than uric acid

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86
Q

Nonsteroidal Anti–inflammatory Drug (NSAID) with analgesic, antipyretic, antiplatelet, and anti–inflammatory properties that irreversibly inhibits COX

A

ASPIRIN (ACETYLSALICYLIC ACID)
▸ Inhibits the formation of PGE, decreases pain and fever, and decreases the synthesis of PGE in the stomach, predisposing to acute gastritis

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87
Q

Used topically for the treatment of Rheumatoid Arthritis because it depletes Substance P

A

CAPSAICIN

▸ Component of chili peppers that impairs the release of Substance P, the potent neurotransmitter for pain sensation

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88
Q

Newly available NSAID, used in the treatment of Rheumatoid Arthritis and other chronic conditions, which decrease the risk of ulcers and GI bleeds

A

CELECOXIB
▸ Similar to Rofecoxib. It selectively blocks COX–2 present only in leukocytes
▸ These agents do not block COX–1 that produces protective gastric prostaglandins
▸ As sulfa drugs, they both cause hypersensitivity

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89
Q

Used in the treatment of acute attacks of Gouty Arthritis, because it impairs leukocyte function

A

COLCHICINE

▸ Inhibits microtubule assembly, and, therefore, leukocyte migration and phagocytosis of uric acid crystals

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90
Q

Used in treatment of transplant patients and patients with autoimmune diseases, as it impairs T–cell production of IL–2

A

CYCLOSPORIN
▸ Binds cyclophilins and inhibits the transcription of cytokine genes
▸ Tacrolimus, binds to immunophilin FK–binding protein and functions similarly
▸ Both have dose–limiting nephrotoxicity

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91
Q

Monoclonal antibody used in the management of patients with renal allografts

A

DACLIZUMAB
▸ Binds to the high affinity IL–2 receptor expressed on activated T–cells
▸ The side effects are minimal compared to agents such as Cyclosporin or Tacrolimus

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92
Q

▸ Used in the treatment of Rheumatoid Arthritis and Inflammatory Bowel Disease (IBD)
▸ A recombinant protein product that inhibits the effects of TNF–alpha

A

ETANERCEPT (IV)
▸ This drug is a fusion between the extracellular domain of TNF–alpha receptor and the Fc portion of an antibody
▸ Similar monoclonal antibody, Infliximab, also binds and inhibits TNF–alpha

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93
Q

Drug used in the treatment of severe Rheumatoid Arthritis, because it decreases lysosomal and macrophage function

A

GOLD SALTS

▸ Side effects include, dermatitis, hematotoxicity and nephrotoxicity

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94
Q

Reversible inhibitors of COX widely used as OTC pain relievers (3)

A

IBUPROFEN, NAPROXEN, PIROXICAM
▸ Same side effects as Aspirin, but more effective analgesics and anti–inflammatories, however they lack Aspirin’s long duration and anti–platelet effects

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95
Q

High–potency NSAID used in the treatment of Gout and Arthritis, and for closure of a Patent Ductus Arteriosus (PDA)

A

INDOMETHACIN

▸ Conversely, PGE can be used to maintain a Patent Ductus Arteriosis (PDA) in congenital cyanotic heart disease

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96
Q

Unlike most Opioid Agonists, this derivative does not cause biliary spasms, and is preferred, therefore, as an analgesic for Pancreatitis and Cholecystitis

A

MEPERIDINE
▸ Causes relaxation of the sphincter of Oddi
▸ All opioids are contraindicated in the case of head injury, because of increased intracranial pressure

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97
Q

Used in the PREVENTION of Migraine Headaches, this Ergot has no value in the TREATMENT of Migraine Headaches

A

METHYLSERGIDE
▸ 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

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98
Q

Uricosuric Agent used in the treatment of Chronic Gout, and also to increase the effective concentration of weakly acidic drugs such as Penicillins

A

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

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99
Q

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

A

RhoGAM
▸ Fetal Rh–positive red blood cells that enter maternal circulation are opsonized by these antibodies, preventing the mother from producing anti–Rh antibodies

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100
Q

Serotonin Agonist used in the treatment of Acute Migraines and Cluster Headaches

A

SUMATRIPTAN

▸ Binds to the 5–HT1D Receptor, causing vasoconstriction of the cerebral vasculature

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101
Q

▸ Notorious for causing teratogenic effects, such as phocomelia
▸ Has gained attention as a potent immunosuppressant

A

THALIDOMIDE
▸ Used in the treatment of SLE, Multiple Myeloma, and Leprosy
▸ Its effects are due to its ability to suppress the production of TNF–alpha

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102
Q

Monoclonal antibody used as an anticoagulant, preventing re–stenosis after coronary angioplasty

A

ABCIXIMAB

▸ Antibody against Glycoprotein IIb/IIIa Receptors on platelets, preventing platelet aggregation

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103
Q

Used in the acute bleeding in patients with hemophilia and other coagulopathies

A

AMINOCAPROIC ACID
▸ An orally active inhibitor of plasminogen activation, thereby inhibiting fibrinolysis
▸ Tranexamic Acid is a similar agent

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104
Q

Recombinant product used in the treatment of Anemia associated with Renal Failure

A

ERYTHROPOIETIN

▸ Also used to treat Anemia associated with Bone Marrow Transplants or Toxic Drug Reactions

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105
Q

Will correct the Anemia but not the neurologic deficits caused by B12 Deficiency

A

FOLIC ACID

▸ Vitamin B12 Deficiency must be ruled out before treating Megaloblastic Anemia with Folic Acid

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106
Q

Rapid–acting, intravenously administered Anticoagulant, used for Acute Myocardial Infarction and prevention of DVT following prolonged immobilization

A

HEPARIN
▸ Binds and activated Antithrombin III, resulting in inactivation of thrombin and other clotting factors
▸ Does not cross the placenta and can be used during pregnancy.
▸ Protamine Sulfate reverses its effects

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107
Q

Used in the management of Sickle Cell Anemia, as well as for various Myeloid Neoplasms

A

HYDROXYUREA
▸ May decrease the incidence of sickle cell crisis, by increasing levels of HbF
▸ It also inhibits DNA synthesis by blocking the conversion of ribonucleotides to deoxyribonucleotides

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108
Q

Recombinately produced Granulocyte–Macrophage Colony–Stimulating Factor (GM–CSF), used in the management of patients undergoing Chemotherapy

A

SARGRAMOSTIM

▸ A similar agent, G–CSF (e.g.,Filgrastim), is used for similar applications, but affects only granulocytes

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109
Q

A bacterial product of Streptococcus pyogenes, used in the treatment of Coronary Artery Thrombosis

A

STREPTOKINASE
▸ Complexes with and catalyzes the conversion of plasminogen to plasmin
▸ It is significantly cheaper, although debatably equivalent, agent to tPA

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110
Q

Platelet antiaggregation, used for the prevention of Transient Ischemic Attacks (TIA) in patients with Aspirin sensitivity

A

TICLOPIDINE
▸ Adenosine Diphosphate (ADP) Receptor Inhibitor
▸ Inhibits fibrinogen binding by preventing Glycoprotein IIb/IIIa Receptors expression on platelets

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111
Q

Created through the use of recombinant DNA technology, this agent is used or Coronary Artery Thrombosis and Ischemic Stroke

A

TISSUE PLASMINOGEN ACTIVATOR (t–PA)

▸ Converts fibrin–bound plasminogen to plasmin, resulting in dissolution of thrombi

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112
Q

Orally administrated Anticoagulant, used in the management and prophylaxis of Venous Thrombosis, Myocardial Infarction, and Stroke

A

WARFARIN

▸ Coumadin compound that interferes with the Vitamin K–dependent carboxylation of clotting factors II, VII, IX, X

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113
Q

Used for the treatment of Traveler’s Diarrhea

A

BISMUTH SUBSALICYLATE
▸ Helps decrease fluid secretion by the bowel
▸ Also used with Metronidazole and Tetracycline for the treatment of H. pylori–associated Peptic Ulcer Disease

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114
Q

Chronic ingestion of this Antacid with Milk can induce the Milk–Alkali Syndrome

A

CALCIUM CARBONATE

▸ Can result in hypercalcemic alkalosis with the development of renal calculi

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115
Q

Used in the treatment of GERD, this Histamine Blocker is associated with Gynecomastia and Galactorrhea

A

CIMETIDINE
▸ The stronger H2 Blockers, Ranitidine and Famotidine do not inhibit the hepatic P–450 system and therefore do no not cause anti–androgenic effects

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116
Q

Prokinetic Agent used in the treatment of upper gastrointestinal dysfunction such as GERD or Gastroparesis with delayed gastric emptying

A

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.

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117
Q

Opioid derivatives used in the treatment of Diarrhea because they suppress gastrointestinal motility

A

DIPHENOXYLATE, LOPERAMIDE
▸ Diphenoxylate is formulated with antimuscarinic alkaloids
▸ Both preparations have minimal abuse potential

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118
Q

This preparation is used to treat Emesis and Nausea associated with Chemotherapy, and contains the active ingredient in Marijuana

A

DRONABINOL
▸ This schedule III drug, which contains Tetrahydrocannabinol (THC), is a controlled substance with approved medical use and moderate potential for dependence

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119
Q

Commonly used pro–emetic agent used in cases of ingestion of caustic substances or mineral oils

A

IPECAC SYRUP

▸ Orally administered substances that act directly on the chemoreceptor trigger zone in the medulla

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120
Q

Among the most popular Antacids used in the United States, neither is absorbed and, therefore, neither causes systemic effects

A

MAGNESIUM HYDROXIDE, ALUMINUM HYDROXIDE

▸ Magnesium Hydroxide also has a strong laxative effect, whereas Aluminum Hydroxide causes constipation

121
Q

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 postrema that trigger vomiting

A

METOCLOPRAMIDE
▸ Functions to facilitate ACh, while antagonizing the action of Dopamine on the enteric nervous system
▸ Side effects include sedation, diarrhea and extrapyramidal symptoms

122
Q

Eicosanoid preparation used to prevent Peptic Ulcers in patients taking high doses of NSAIDs for conditions such as Rheumatoid Arthritis

A

MISOPROSTOL
▸ This prostaglandin (PGE) analog decreases gastric acid production and increases mucous production, protecting the lining of the stomach

123
Q

Proton Pump Inhibitor used in the treatment of GERD, Gastric and Duodenal Ulcers, H. pylori Gastritis, and Zollinger–Ellison Syndrome (Gastrinoma)

A

OMEPRAZOLE

▸ Irreversibly inhibits the H+/K+ ATPase on the luminal side of parietal cells

124
Q

Central–acting Anti–emetic used to control post–operative vomiting and vomiting in chemotherapy patients

A

ONDANSETRON

▸ 5–HT3 inhibitor that functions at the chemoreceptive area of the area postrema

125
Q

Used in the treatment of Peptic Ulcers, because it polymerizes and selectively coats necrotic ulcerated tissue

A

SUCRALFATE
▸ Requires an acidic environment to polymerize, and, therefore, cannot be used in the presence of Antacids or H2 Blockers

126
Q

Beta–Adrenergic Antagonists used in the treatment of Hypertension for patients with Asthma or COPD, and Smokers (3)

A

ACEBUTOLOL, ATENOLOL, METOPROLOL

▸ Selective Beta–1 Blockers that decrease blood pressure, with no bronchoconstriction at low doses

127
Q

Prototypic Adrenergic Agonist, available as an inhaler, used for the management of Bronchospasm in Asthmatics

A

ALBUTEROL

▸ Other selective Beta–2 Agonists include Metaproterenol, Terbutaline, and Salmeterol.

128
Q

▸ Synthetic glucocorticoid that readily penetrates the airway mucosa
▸ Used in the management of Asthma

A

BECLOMETHASONE
▸ Beclomethasone and a related agent, Budesonide, have very short half–lives in the bloodstream, and, therefore, cause less systemic effects than other glucocorticoids

129
Q

Stabilizes Mast Cell and Basophil Membranes, preventing the release of Histamine in Asthmatics

A

CROMOLYN SODIUM

▸ Used in Prophylaxis only, not for the treatment of Acute Asthma Attacks

130
Q

Opioid Agonist available in many over–the–counter cough syrups

A

DEXTROMETHORPHAN
▸ Antitussive Agent that depresses the cough center in the medulla
▸ Unlike Dextromethorphan, Codeine provides analgesia and has a higher abuse potential

131
Q

Antihistaminics used for treatment of allergic conditions (Hay Fever, Urticaria, Atopy), as well as for the treatment of Motion Sickness

A

DIPHENHYDRAMINE, CHLORPHENIRAMINE
▸ Inhibit the binding of Histamine to H1 Receptors
▸ Such older agents have anticholinergic effects, contributing to sedative side effects

132
Q

Non–sedating Antihistaminics used in the treatment of Allergy

A

FEXOFENADINE, LORATADINE

▸ These Second–Generation Antihistaminics do not readily enter the CNS, preventing sedation

133
Q

Aerosolized Antimuscarinic Agent, used in the treatment of COPD and Asthma

A

IPRATROPIUM
▸ Not as effective as Beta–2 Agonists
▸ Dry mouth is a major side effect

134
Q

Long–acting Beta–2 Agonist used for Prophylaxis of Asthma

A

SALMETEROL
▸ This agent works for 12 hours or more
▸ It may cause tremors and arrhythmias

135
Q

A Methylxanthine used in the treatment of Asthma for its brochodilatory effects

A

THEOPHYLLINE
▸ Inhibits Phosphodiesterase, thereby inhibiting the degradation of cAMP to AMP
▸ Other Methylxanthines include Caffeine and Theobromine found in cocoa

136
Q

Used in the treatment of Asthma, selectively inhibiting Leukotriene Synthesis

A

ZILEUTIN

▸ Leukotrienes can also be inhibited by the LTD4 and LTE4 Antagonists Zafirlukast and Montelukast

137
Q

Oral Hypoglycemic Agent that functions within the intestinal lumen, decreasing Postprandial Hyperglycemia, although there are no effects on fasting sugar

A

ACARBOSE

▸ Inhibits Alpha–Galactosidase, an enzyme required for rapid absorption of most dietary sugars

138
Q

These compounds reduce bone resorption and formation, and are used in the treatment of Osteoporosis (Postmenopausal, Senile, or Glucocorticoid–induced) and Paget Disease

A

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

139
Q

Used in the treatment of Hyperprolactinemia, e.g., due to a Pituitary Adenoma

A

BROMOCRIPTINE

▸ Ergot Alkaloid with dopaminergic activity, inhibiting the release of Prolactin

140
Q

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

A

CALCITONIN
▸ Used in the treatment of Acute Hypercalcemia and Paget Disease
▸ Administered intranasally or by injection
▸ Salmon type has longer t1/2

141
Q

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

A

CLOMIPHENE

▸ Blocks negative feedback to the pituitary, increasing the release of FSH and LH to stimulate ovulation

142
Q

A Synthetic Analog of ACTH used to diagnose patients with abnormalities of Cortisol production (Addison’s Disease)

A

COSYNTROPIN
▸ Proteolytic cleavage of pre–pro–opiomelanocortin (pre–POMC) forms ACTH and Melanocyte–Stimulating Hormone (MSH), as well as Beta–Endorphin and Metenkephalin

143
Q

Used in the treatment of Endometriosis and Fibrocystic Disease of the Breast

A

DANAZOL

▸ Inhibits several P450 enzymes involved in gonadal steroid synthesis

144
Q

An Anti–Diuretic Hormone (ADH) Receptor Agonist used for the treatment of Pituitary Diabetes Insipidus (2)

A

VASOPRESSIN, DESMOPRESSIN
▸ Desmopressin is a V2–Selective Agonist that facilitates water reabsorption from the collecting tubules
▸ Vasopressin is both a V1 & V2 Agonist; its V1 activity increases vascular smooth muscle tone and, therefore, is used for treatment of Esophageal Varices

145
Q

Use of this estrogen compound by pregnant women has been associated with the development of Clear Cell Adenocarcinoma of the Vagina in their daughters

A

DES (DIETHYLSTILBESTROL)

▸ May be used as Post–coital (Morning After) Birth Control, and for the treatment of Testicular Tumors

146
Q

Synthetic Estrogen with high oral availability, used in contraceptive pills as well as in Hormone Replacement Therapy (HRT)

A

ETHINYL ESTRADIOL, MESTRANOL
▸ 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

147
Q

Antiandrogenic compound used in the treatment of Benign Prostatic Hyperplasia and Alopecia

A

FINASTERIDE

▸ Inhibits 5–Alpha–Reductase, and thus conversion of Testosterone to Dihydrotestosterone (DHT)

148
Q

Used for Mineralocorticoid Deficiency, this agent has a long duration of action, and is a naturally occurring precursor to Aldosterone

A

FLUDROCORTISONE

▸ Used in conjunction with glucocorticoids in post–adrenalectomy therapy

149
Q

This Ultra–rapid–acting Human Insulin administered immediately before meals

A

INSULIN LISPRO

▸ An altered form of Insulin that enters the circulation more rapidly than Crystalline Zinc (Regular) Insulin

150
Q

A Synthetic Thyroid Hormone used in the treatment of Hypothyroidism as seen in Hashimoto’s Thyroiditis, Myxedema, and in patients on Lithium

A

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, used less frequently

151
Q

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

A

METFORMIN
▸ Biguanide compound that functions by increasing peripheral glycolysis, and, therefore, hepatic gluconeogenesis, resulting in a decrease in serum glucose levels

152
Q

Abortifacient steroid receptor antagonist known as the “Morning After” Pill

A

MIFEPRISTONE (RU486)

▸ Blocks the binding of Progesterone to cytoplasmic receptors, preventing successful implantation

153
Q

Synthetic Progesterone Analog used in oral contraceptives and implantable contraceptive devices

A

NORGESTREL
▸ Norgestrel and similar agent, such as Norethindrone and Medroxyprogesterone, may be used in Hormone Replacement Therapy (HRT), and to prevent abnormal uterine bleeding

154
Q

A Synthetic Analog of Somatostatin, used in the treatment of many Endocrine Tumors, including Carcinoid, Gastrinoma, and Somatropic Pituitary Adenoma

A

OCTREOTIDE

▸ This octapeptide is used instead of Somatostatin, because it has a longer half–life

155
Q

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

A

OXYTOCIN
▸ Stimulates contraction of uterine smooth muscle for labor
▸ Stimulates contraction of the myoepithelial cells of the mammary glands to eject milk

156
Q

Oral agent used in the treatment of Hyperthyroidism

A

PROPYLTHIOURACIL (PTU)
▸ Inhibits the iodination and coupling reactions of thyroid hormone synthesis
▸ Methimazole is also used, although it can cross the placenta and enter breast milk

157
Q

This Estrogen Partial Agonist is used to prevent Osteoporosis in postmenopausal women

A

RALOXIFENE
▸ It also increases serum HDL, protecting against atherosclerosis and heart disease
▸ Unlike another Selective Estrogen Receptor Modulator (SERM), Tamoxifen, it does not increase the risk of endometrial carcinoma

158
Q

This Insulin Secretagogue has rapid onset, but shorter duration of action than Sulfonylureas

A 
REPAGLINIDE
▸ Belongs to a class of drugs known as Meglitinides, which facilitate Insulin release from pancreatic beta cells by binding to potassium channels
159
Q

These agents increase cell sensitivity to Insulin, by stimulating the Peroxisome Proliferator–Activated Receptor gamma (PPARgamma) nuclear receptor (2)

A

ROSIGLITAZONE, PIOGLITAZONE
▸ PPARgamma 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

160
Q

Oral Hypoglycemic Agents used to stimulate the release of Endogenous Insulin from beta cells

A

SULFONYLUREAS (GLYBURIDE, GLIPIZIDE)
▸ Stimulate the closure of potassium channels, resulting in depolarization of beta cells and release of preformed Insulin in vesicles

161
Q

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

A

ULTRALENTE INSULIN
▸ Supplemented throughout the day with Insulin Lispro
▸ A modified version of Human Insulin, Insulin Glargine, has an even longer duration of action

162
Q

Oral, topical, and IV preps are available, used to reduce symptomatology of HSV Infection, although it does not inhibit the reactivation of herpes

A

ACYCLOVIR

163
Q

Guanosine Analog is activated by Thymidine Kinase of herpes virus (HSV, VZV, EBV) and function as chain terminator when incorporated into viral DNA during replication

A

ACYCLOVIR

164
Q

▸ Used for Prophylaxis of Influenza A and Rubella Viral Infection if given within 48 hr of exposure
▸ Also used in treatment of Parkinson’s
▸ Not effective against Influenza B

A

AMANTADINE

165
Q

Inhibit fusion of viral particles within an endosome in a cell (2)

A

AMANTADINE, RIMANTADINE

166
Q

Longer half life than Amantadine with same action

A

RIMANTADINE

167
Q

Ineffective against anaerobes, due to the requirement for oxygen to be taken up by the organism

A

AMINOGLYCOSIDES

GENTAMICIN, NEOMYCIN, AMIKACIN, TOBRAMYCIN, STREPTOMYCIN

168
Q

▸ Bactericidal Inhibitors of mRNA Translation at the 30S ribosome
▸ These agents are associated with significant nephrotoxicity and ototoxicity

A

AMINOGLYCOSIDES

GENTAMICIN, NEOMYCIN, AMIKACIN, TOBRAMYCIN, STREPTOMYCIN

169
Q

Polyene Antifungal Agent used for the treatment of Systemic Mycosis and intrathecally for the treatment of Fungal Meningitis

A

AMPHOTERICIN B

170
Q

▸ Disrupts fungal membranes by binding to Ergosterol, which induces pore formation
▸ SE: chills, fever, hypotension, dose–limiting nephrotoxicity (all of which are less severe when using liposomal formulations)

A

AMPHOTERICIN B

171
Q

▸ Extended Spectrum Penicillin used to treat infections with GN organisms such as Haemophilus, E. coli, Listeria, Proteus, and Salmonella
▸ Often administered with Penicillinase Inhibitors

A

AMPICILLIN

172
Q

Similar to Ampicillin, but greater oral bioavailability and decreased GI irritability

A

AMOXICILLIN

173
Q

Works similarly to Penicillins and Cephalosporins, this Monobactam is resistant to Beta–Lactamases, and displays no cross–allergenicity with Penicillins

A

AZTREONAM

174
Q

▸ Ineffective against GP or anaerobic bacteria

▸ Works synergistically with Aminoglycosides against GNR

A

AZTREONAM

175
Q

Inhibitor of bacterial cell wall synthesis, is available as a topical preparation in many OTC antibacterial ointments

A

BACITRACIN

176
Q

▸ Peptide Antibiotic inhibits cell wall synthesis in GP organisms
▸ Causes severe nephrotoxicity if used systematically

A

BACITRACIN

177
Q

▸ Extended–Spectrum Penicillins

▸ Useful against Pseudomonas and Enterobacter

A

CARBENICILLIN, PIPERACILLIN, TICARCILLIN

178
Q

Can be used with Penicillinase Inhibitors and work synergistically with Aminoglycosides

A

CARBENICILLIN, PIPERACILLIN, TICARCILLIN

179
Q

▸ Used for treatment of septic meningitis

▸ This Cephalosporin has good penetration into CNS

A

CEFTRIAXONE

180
Q

▸ 3rd Generation Cephalosporin

▸ Coverage against Bacterial Meningitis – Strep pneumoniae, H. influenzae, Neisseria meningitides

A

CEFTRIAXONE

181
Q

Cyanosis and CV collapse in premature neonates deficient in hepatic gluconosyltransferase (Gray Baby Syndrome)

A

CHLORAMPHENICOL

182
Q

Bacteriostatic Inhibitor of protein synthesis – blocks peptidyl transferase activity at 50S ribosome

A

CHLORAMPHENICOL

183
Q

▸ Associated myelosuppression, and rarely an idiosyncratic, irreversible aplastic anemia
▸ Rarely used systematically due to inhibition of RBC maturation; available as topical

A

CHLORAMPHENICOL

184
Q

▸ Primary drug used for acute attacks and prophylaxis of malarial infection
▸ Resistance is common

A

CHLOROQUINE

185
Q

▸ Kills parasites within erythrocytes (Schizonticidal)

▸ It disrupts hemoglobin breakdown, with the accumulation of heme, which is toxic to the organism

A

CHLOROQUINE

186
Q

Administered with Penicillins to enhance their antimicrobial effects

A

CLINDAMYCIN

187
Q

▸ Bacteriostatic inhibitor of protein synthesis, methylating the 50S ribosomal subunit
▸ Used in treatment of serious anaerobic infections due to Bacteroides

A

CLINDAMYCIN

188
Q

Used in combined regimens for treatment of HIV Infection, associated with a dose–limiting pancreatitis

A

DIDANOSINE (DDI)

189
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

A

▸ Zidovudine (ZDT)
▸ Salcitabine (ddC)
▸ Lamivudine (3TC)
▸ Stavudine (d4T)

190
Q

NRTI that also inhibits Reverse Transcriptase of HBV

A

LAMIVUDINE (3TC)

191
Q

▸ Widely used antibiotic

▸ SE include GI irritation and hypersensitivity–based acute cholestatic hepatitis

A

ERYTHROMYCIN

▸ Bacteriostatic inhibitor of protein synthesis, functioning on 50S ribosome

192
Q

Good coverage against Mycoplasma, Corynebacterium, Chlamydia, Legionella, and Bordetella

A

MACROLIDES
▸ Erythromycin
▸ Azithromycin
▸ Clarithromycin

193
Q

Can cause tendon damage in adults, is contraindicated in children and pregnant women because of damage to developing cartilage

A

FLUOROQUINOLONES
▸ Ciprofloxacin
▸ Norfloxacin

194
Q

Bactericidal inhibitor of DNA Gyrase, used for GNR, Neisseria

A

FLUOROQUINOLONES
▸ Ciprofloxacin
▸ Norfloxacin

195
Q

Imidazole Antifungal used for the treatment of fungal meningitis, because it can cross the blood–brain barrier

A

FLUCONAZOLE

196
Q

Inhibits the formation of Ergosterol, lacks the anti–endocrine effects seen with Ketoconazole

A

FLUCONAZOLE

197
Q

Prophylaxis against Cryptococcus neoformans, effective in the treatment of Esophageal and Oropharyngeal Candidiasis

A

FLUCONAZOLE

198
Q

Backup drug used for treatment of CMV infection in immunocompromised patients, when resistance to Ganciclovir develops

A

FOSCARNET

199
Q

▸ Does not require phosphorylation by viral kinases and inhibits viral DNA polymerase at different site than Ganciclovir
▸ Not metabolized by viral transferases, which render Ganciclovir ineffective

A

FOSCARNET

200
Q

Used for the treatment of Retinitis and other infections associated with CMV

A

GANCICLOVIR

201
Q

▸ Gaunosine Analog converted by CMV to a triphosphorylated form which inhibits the viral polymerase
▸ Given IV – good penetration to the eye and CNS
▸ Causes neutropenia, leucopenia, thrombocytopenia

A

GANCICLOVIR

202
Q

Given orally, Antifungal that accumulates in keratinized tissue and is effective against dermatophyte infections, such as ringworm (Tinea)

A

GRISEOFULVIN

203
Q

Binds tubulin, interfering with MT function, inhibits mitosis

A

GRISEOFULVIN

204
Q

Broad–Spectrum Beta–Lactamase–Resistant Carbapenem, given in conjunction with Cilastatin

A

IMIPENEM

205
Q

▸ Used against GPC, GNR, anaerobes

▸ Metabolized by Renal Dihydropeptidase, which is blocked by coadministration of Cilastatin

A

IMIPENEM

206
Q

Protease Inhibitors used in combined treatment regimens for HIV infection

A

Indinavir, Ritonavir, Saquinavir, Nelfinavir

207
Q

▸ Agents inhibit the protease encoded by HIV pol gene and required for the production of infectious virions
▸ Metabolized by CYP450

A

Indinavir, Ritonavir, Saquinavir, Nelfinavir

208
Q

▸ This agent is recommended for 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

A

ISONIAZID (INH)

209
Q

▸ 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

A

ISONIAZID (INH)
▸ Due to the emergence of multidrug–resistant strains of Mycobacterium tuberculosis, multidrug regimens also include Ethambuto, Pyrazinamide, Rifampin, and Streptomycin.

210
Q

Antihelminthic Agent used for the treatment of River Blindness (Onchocerca volvulus) and Threadworm Infection (Strongyloides stercoralis)

A

IVERMECTIN

211
Q

Increases GABA–mediated neourotransmission, but since it does not cross the human blood–brain barrier, it selectively affects the nematode, resulting in paralysis of the worm

A

IVERMECTIN

212
Q

▸ Used for the treatment of Mycotic Infections

▸ These agents inhibit hormone production and result in gynecomastia

A

AZOLES
▸ Ketoconazole
▸ Itraconazole
▸ Fluconazole

213
Q

▸ These drugs interfere with fungal cell wall synthesis by inhibiting the 14–alpha–demethylation of lanosterol
▸ The demethylation is catalyzed by the cytochrome P450 system

A

AZOLES
▸ Ketoconazole
▸ Itraconazole
▸ Fluconazole

214
Q

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

A

MEBENDAZOLE

215
Q

Functions by inhibiting microtubule synthesis and glucose uptake in helminthes

A

MEBENDAZOLE

▸ Related drugs such as Albendazole and Thiabendazole and alternatives

216
Q

▸ Narrow–Spectrum, Penicillinase–Resistant Beta–Lactam Antibiotics
▸ Used to treat Penicillin–resistant Staph aureus

A

Methicillin, Nafcillin, Dicloxacillin

217
Q

Bulkier R–groups on the Penicillin backbone prevent degradation by Penicillinases

A

Methicillin, Nafcillin, Dicloxacillin

218
Q

Antiprotozoal Agent used in the treatment of Amebiasis, Trichomoniasis, and Giardiasis, as well as for Pseudomembranous Colitis

A

Metronidazole

219
Q

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

A

Metronidazole

220
Q

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

A

Neomycin

221
Q

▸ Prevents the growth of GI flora and accumulation of nitrogenous microbial metabolites, which contribute to the development of hepatic encephalopathy
▸ Too toxic to be administered IV, but often used topically in the OTC antibiotic ointments

A

Neomycin

222
Q

Non–nucleoside Reverse–transcriptase Inhibitors used in the management of HIV Infection

A

Nevirapine, Delavirdine, Efavirenz

223
Q

▸ Drugs bind to a unique site on reverse transcriptase, there is no cross–resistance with the NRTIs
▸ The NNRTIs are all metabolized by the P450 system

A

Nevirapine, Delavirdine, Efavirenz

224
Q

Trypanosomicidal drug used for the treatment of Chagas Disease

A

Nifurtimox

225
Q

Drugs used to treat African trypanosomiasis include Pentamidine, Suramin, Melarsoprol

A

Nifurtimox

226
Q

Urinary antiseptic that requires acidification and therefore, is ineffective systematically, although toxic levels can accumulate in patients with renal failure

A

Nitrofurantoin

227
Q

Can cause GI side effects, rash, and hemolysis in G6PD deficiency patients

A

Nitrofurantoin

228
Q

Swish and swallow treatment for Oral Candidiasis, or topically for the treatment of Diaper Rash

A

Nystatin

229
Q

Disrupts fungal membrane permeability by binding to Ergosterol

A

Nystatin

230
Q

Orally active Antiviral drug used to decrease the duration and symptoms of Influenza A symptoms

A

OSELTAMIVIR
▸ Zanamivir is a similar drug, but administered intranasally
▸ Both drugs function as neuraminidase inhibitors, preventing the spread of virus from cell to cell

231
Q

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

A

Penicillins

232
Q

▸ Mechanism is similar to Cephalosporins is nearly identical

▸ Major side effects: hypersensitivity with urticaria, and rarely, anaphylaxis leading to life–threatening asphyxiation

A

Penicillins

233
Q

Antibiotic disrupts bacterial membranes and is often too toxic to be administered systematically, although it is safe topically

A

Polymixin B

234
Q

▸ Acts as a cationic detergent that disrupts the membrane

▸ Systemic use causes neurotoxicity and acute tubular necrosis

A

Polymixin B

235
Q

Primary drug used for the treatment of Trematode (Fluke) and Cestode (Tapeworm) Infections

A

Praziquantel

236
Q

Increases calcium permeability in the worm, resulting in paralysis

A

PRAZIQUANTEL
▸ Niclosamide, which functions by uncoupling oxidative phosphorylation (inhibiting ATP production) or by activating ATPases, often is used with this drug in cestode infections

237
Q

Antihelminthic Agent, often used with Mebendazole for the treatment of roundworm, pinworm, and hookworm infections

A

Pyrantel Pamoate

238
Q

Stimulates nicotinic receptors in the nematode, resulting in a spastic paralysis

A

Pyrantel Pamoate

239
Q

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

A

Quinine

240
Q

▸ Blocks DNA replication and RNA transcription in P. falciparum within erythrocytes

A

QUININE
▸ A common SE is cinchonism, a constellation of symptoms including headache, vertigo, blurred vision, and tinnitus
▸ A related drug, Mefloquine, has fewer SE and is used as prophylaxis in chloroquine–resistant areas

241
Q

Administered as an aerosol, this drug is used for the treatment of RSV

A

Ribavirin

242
Q

▸ Guanosine Analog that inhibits formation, the capping of viral mRNA, and viral RNA–dependent RNA pol activity
▸ Also used for the management of viral hemorrhagic fevers and Hepatitis C Infection

A

Ribavirin

243
Q

▸ Rarely used alone, except for the treatment of meningococcal carrier state
▸ This drug imparts a red–orange color secretions

A

Rifampin

244
Q

▸ Inhibits DNA–Dependent RNA Polymerase

▸ Often used in a combined drug regimen for Mycobacterium tuberculosis because of rapid resistance if used alone

A

Rifampin

245
Q

This class of antibiotics inhibits protein synthesis and is effective in the treatment of MRSA and Vancomycin–Resistant Enterococci (VRE)

A

STREPTOGRAMINS
▸ Synercid is a mixture of Quinupristin and Dalfopristin
▸ Use associated with arthralgias and myalgias, as well as inhibition P450 enzymes

246
Q

▸ Synercid is a mixture of Quinupristin and Dalfopristin

▸ Use associated with arthralgias and myalgias, as well as inhibition P450 enzymes

A

Streptogramins

247
Q

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

A

Tetracycline

248
Q

▸ Broad–Spectrum bacteriostatic drug that inhibits the 30S ribosome and thus protein synthesis
▸ Provides good coverage against Mycoplasma, Chlamydia, Rickettsia, and Vibrio

A

Tetracycline

249
Q

▸ These two drugs create a block in successive reactions for folate synthesis
▸ Also often used to treat UTIs

A

Trimethoprin & Sulfamethoxazole

TMP–SMX

250
Q

▸ Blocks bacterial DHF–R and can cause megaloblastic anemia
▸ Blocks dihydropteroate synthase and can cause hypersensitivity reactions and hemolysis in patients with G6PDH deficiency

A

Trimethoprim, Sulfamethoxazole

TMP–SMX

251
Q

Rapid IV infusion is associated with diffuse flushing (Red Man Syndrome)

A

Vancomycin

252
Q

▸ Treatment of MRSA, Pseudomembranous Colitis due to C. diff

▸ SE can be limited by infusion over prolonged period and co–administration of antihistamines

A

Vancomycin

253
Q

Commonly used as part of HAART, this HIV drug is used for prophylaxis of needlestick transmission and of transmission to neonates from infected mothers during birth

A

Zidovudine (ZDT)

254
Q

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

A

Zidovudine (ZDT)

255
Q

Inhibits the enzyme Aromatase and is used for the treatment of estrogen–dependent breast cancer

A

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

256
Q

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

A

A: Bleomycin. (The drug is a mixture of glycoproteins that results in the production of free radicals after binding to DNA, creating single–& double–stranded breaks. This G2 phase inhibitor is part of the ABVD regimen [adriamycin, bleomycin, vinblastine, & decarbazine] for Hodgkin disease.)

257
Q

Q: Highly lipophilic nitrosoureas that readily cross the blood–brain barrier and are used for the treatment of many brain tumors

A

A: Carmustine (BCNU), Lomustine (CCNU). (These alkylating agents result in DNA cross–linking and strand breaks)

258
Q

Q: Platinum–containing compound used in the treatment of testicular and lung carcinomas.

A

A: 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)

259
Q

Q: Alkylating agent used for the treatment of non–Hodgkin lymphoma and breast and ovarian carcinomas

A

A: Cyclophosphamide. (The major side effect, hemorrhagic cystitis, may be decreased by vigorous hydration and the use of mesna)

260
Q

Q: Part of the AVBD regimen, an antibiotic–type compound used in the treatment of myelomas, sarcomas, and lymphomas

A

A: Doxorubicin (Adriamycin). leukemia [AML].)(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 )

261
Q

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

A

A: Etoposide. (G2 phase–specific inhibition, resulting in double–stranded DNA breaks and degradation)

262
Q

Q: Inhibits thymidylate synthase, resulting in thymineless death, and is used for the treatment of colon cancer and superficial tumors, such as basal cell carcinoma.

A

A: Fluorouracil (5–FU). (This S–phase antimetabolite causes myelosuppression)

263
Q

Q: Androgen receptor antagonist, used for the treatment of carcinoma of the prostate

A

A: Flutamide. (Used to antagonize residual androgens after orchiectomy; side effects include gynecomastia and libido changes)

264
Q

Q: Recombinantly produced cytokine, used for the treatment of hairy cell leukemia

A

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

265
Q

Q: Gonadotropin–releasing hormone (GnRH) agonists, used for the treatment of metastatic carcinoma of the prostate

A

A: Leuprolide, Goserelin, Nafarelin. (May also 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)

266
Q

Q: Purine metabolites, used for the treatment of leukemias and lymphomas

A

A: Mercaptopurine (6–MP), Thioguanine (6–TG). (Requires activation by hypoxanthine–guanine phosphoribosyltransferase [HGPRT], and inhibits many enzmes involved in purine metabolism)

267
Q

Q: Folic acid analog, used for the treatment of leukemias, non–Hodgkin lymphoma, rheumatoid arthritis, and therapeutic abortions.

A

A: Methotrexate. (S phase inhibitor of dihydrofolate reductase, leading to decreased DNA and protein synthesis; the accompanying myelosuppression can be treated with leucovorin).

268
Q

Q: Microtubule stabilizing agent, used for the treatment of ovarian and breast carcinomas.

A

A: Paclitaxel. (Derived from the yew tree, this M phase agent prevents the mitotic spindle from breaking down and thus inhibits completion of anaphase).

269
Q

Q: Glucocorticoid used for the treatment of leukemias and lymphomas, as well for rheumatoid arthritis and asthma.

A

A: Prednisone. (Triggers apoptosis and can lead to hypercortisolism with Cushing–like symptoms. Drug must be tapered gradually to prevent life–threatening adrenal insufficiency).

270
Q

Q: Monoclonal antibody used for the treatment of low–grade non–Hodgkin lymphoma.

A

A: Rituximab. (Binds to the CD20 antigen on B cells; adverse reactions are associated with infusion, and include fever, chills, headache, and nausea).

271
Q

Q: Primary agent used in the treatment of estrogen receptor–positive breast cancer.

A

A: Tamoxifen. (An estrogen receptor partial agonist, which may increase the risk of endometrial carcinoma).

272
Q

Q: Monoclonal antibody used for the treatment of metastatic breast cancer.

A

A: Trastuzumab. (Binds to the receptor tyrosine kinase Erb–B2 [HER–2], overexpressed on some breast cancers).

273
Q

Q: Vinca alkaloid used as part of the MOPP regimen for lymphomas, Wilms tumor, and choriocarcinomas.

A

A: 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 use of adriamycin, bleomycin, vinblastine, and dacarbazine whereas the MOPP regimen includes the use of mechlorethamine, Oncovin [vincristine], procarbazine, and prednisone.)

274
Q

Q: Used to treat the ingestion of suicidal doses of acetaminophen.

A

A: N–acetylcysteine. (Given early, it may protect from the development of fulminant hepatic failure).

275
Q

Q: Antispasmodic used for the treatment of malignant hyperthermia and neuroleptic malignant syndrome.

A

A: Dantrolene. (Decreases the release of calcium from the sarcoplasmic reticulum).

276
Q

Q: Used for the treatment of acute iron toxicity.

A

A: Deferoxamine. (Rapid infusion has been associated with hypotensive shock).

277
Q

Q: Fab fragment antibody used for the treatment of digitalis toxicity.

A

A: Digibind. (Treatment also includes the correction of Mg2+ and K+, as well as lidocaine for induced arrhythmias).

278
Q

Q: Agent used to treat heavy metal poisoning due to lead, arsenic, and mercury.

A

A: Dimercaprol. (Given parenterally, it chelates metals, preventing them from damaging proteins; succimer is an orally available derivative used for similar applications).

279
Q

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

A

A: Ethylene Glycol. (A major component of antifreeze, toxicity is managed by the administration of ethanol).

280
Q

Q: Used in the event of benzodiazepine overdose.

A

A: Flumazenil. (This benzodiazepine derivative antagonizes the actions of benzodiazepines and zolpidem, although it does not block the actions of barbiturates).

281
Q

Q: Intoxicant that can cause retinal damage and blindness along with metabolic acidosis and coma.

A

A: Methanol. (Damage is due to the conversion to formaldehyde by the liver; the treatment includes ethanol, which competes for alcohol dehydrogenase.)

282
Q

Q: Used to treat the symptoms of opioid overdose.

A

A: Naltrexone, Naloxone. (Pure antagonists, primarily of mu opioid receptors).

283
Q

Q: Anticholinesterases used as insecticides and as possible agents of chemical warfare, inducing motor paralysis, respiratory depression and convulsions.

A

A: Organophosphates (Isoflurophate/Echothiophate/Parathion). (Antidote includes the use of atropine and acetylcholinesterase regenerators, such as pralidoxime).

284
Q

Q: Derivative of penicillin with the ability to chelate copper ions, used for the treatment of copper toxicity.

A

A: Penicillamine. (Also used for the treatment of Wilson disease, and an adjunct therapy for rheumatoid arthritis).

285
Q

Q: Drugs that cause significant ototoxicity and nephrotoxicity.

A

A: 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).

286
Q

Q: Drugs that lead to pulmonary fibrosis and subsequent restrictive lung disease.

A

A: Bleomycin (Antineoplastic), Amiodarone (Class 1A 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]).

287
Q

Q: Drugs that cause gynecomastia.

A

A: Cimetidine (Antiulcer), Ketoconazole (Antifungal), Spironolactone (Antihypertensive). (All compete for androgen receptors, leading to antiandrogenic effects).

288
Q

Q: Common drugs that inhibit hepatic P450 system.

A

A: 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).

289
Q

Q: Drugs that can cause massive hepatic necrosis.

A

A: Halothane (Anesthetic), Acetaminophen (Analgesic), Valproic Acid (Anticonvulsant) (Histologically, damage to the liver is indistinguishable from that caused by chronic viral hepatitis).

290
Q

Q: Drugs that cause a systemic lupus erythematosus (SLE)–like syndrome.

A

A: Hydralazine (Vasodilator), Procainamide (Class 1A Antiarrhythmic), Isoniazid (Antituberculoid), Phenytoin (Anticonvulsant). (Symptoms include arthralgias, myalgias, skin rashes, and fever).

291
Q

Q: Drugs that inhibit microtubule function.

A

A: 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.)

292
Q

Q: Drugs that cause a disulfram–like reaction.

A

A: Metronidazole (Antibiotic), Certain Cephalosporins (Antibiotic), Procarbazine (Antineoplastic). (Cause flushing, headache, nausea, sweats, hypotension, and confusion).

293
Q

Q: Drugs that cause cutaneous flushing on administration.

A

A: Niacin (Antihyperlipidemic), Calcium Channel Blockers, Adenosine (Antiarrhythmic), Vancomycin (Antibiotic). (Often this side effect can be controlled by slow infusion or coadministration with histamine blockers).

294
Q

Q: Bactericidal antibiotics.

A

A: Penicillins, Cephalosporins, Vancomycin, Aminoglycosides, Fluoroquinolones, Metronidazole. (Most of the other antibiotics are bacteriostatic).

295
Q

Q: Drugs that induce the hepatic P450 system.

A

A: 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).

296
Q

Q: Drugs that cause a Stevens–Johnson syndrome, a febrile, erosive hemorrhagic crusting on the lips and oral mucosa of children.

A

A: 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 erytheme multiforme, with macules, papules, vesicles and bullae).

297
Q

Q: Drugs that can cause hemolysis in patients with glucose–6 phosphate dehydrogenase (G6PDH) deficiency.

A

A: Sulfonamides (Antibiotic), Isoniazid (Antituberculoid), Primaquine (Antimalarial). (In patients with G6PDH 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).

298
Q

Q: Drugs that cause photosensitivity.

A

A: Tetracycline (Antibiotics), Amiodarone (Class 1A Antiarrhythmic), Sulfonamides (Antibiotics).(Barbiturates can precipitate photosensitivity in patients with acute intermittent porphyria).

USMLE (16 decks)

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