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Flashcards in BRS Pharm Deck (298)
1

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

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".

2

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

3

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

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

4

Indirect–acting sympathomimetic used in OTC nasal decongestants

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

5

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

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

6

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

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

7

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

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

8

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

9

▸ Used to treat hypertension and urinary retention
▸ First–dose syncope is a significant side effect associated with this drug

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

10

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

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

11

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 is has a shorter duration of action

12

Used to prevent motion sickness and delivered by a transdermal patch

SCOPOLAMINE
▸ Competitive cholinergic antagonist with sedating and amnestic effects

13

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 occur in some patients when used with Halothane

14

Nondepolarizing neuromuscular ganglionic blockers used in surgical anesthesia (3)

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

15

▸ 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

16

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

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

17

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

18

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

19

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

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

20

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 in pregnancy

21

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

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

22

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)

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

23

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

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–

24

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

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

25

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

26

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

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

27

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

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

28

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

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

29

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

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

30

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

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

31

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

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.

32

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

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

33

▸ Used for the Tx of recurrent ventricular arrhythmias
▸ Many of these agents can precipitate torsade de pointe arrhythmias

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

34

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

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

35

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

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

36

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

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

37

Agents that decrease triglycerides dramatically by stimulating lipoprotein lipase

GEMFIBROZIL, FENOFIBRATE, CLOFIBRATE
▸ CLOFIBRATE has been associated with GALLSTONES and HEPATOBILIARY NEOPLASMS

38

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

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

39

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

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

40

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

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

41

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

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

42

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

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

43

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

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

44

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

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

45

Inhibits 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 CREATINE KINASE from skeletal muscle, and, rarely, RHABDOMYOLYSIS

46

Intermediate–acting Benzodiazepine used for the Tx 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–HT(1A) RECEPTORS w/ MINIMAL ABUSE POTENTIAL

47

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

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

48

Orally active anti–spasmodic agent

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

49

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

50

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

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

51

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

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

52

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

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

53

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

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

54

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

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

55

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

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

56

The only local anesthetic with vasoconstrictor activity

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

57

▸ Used for Tx of anxiety and ethanol dependence
▸ Also a primary agent in the Tx of status epilipticus

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

58

Used in the Tx of Parkinson 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

59

Preferred agent in the Tx of absence seizures

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

60

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

61

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

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

62

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

63

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

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

64

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

65

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

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

66

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

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

67

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

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

68

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 usually is ADMINISTERED WITH AN IV ANESTHETIC such as THIOPENTAL, and is commonly used in DENTAL PROCEDURES

69

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

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

70

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

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

71

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

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

72

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

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

73

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

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

74

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

SELEGILINE
▸ Inhibits MAO–B, which selectively degrades DOPAMINE

75

Ultra–short–acting barbiturate used IV 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

76

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

77

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

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

78

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

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

79

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

AMPHETAMINES
▸ Function as an indirect sympathomimetic by releasing stored catecholamines

80

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

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

81

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

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

82

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

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

83

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

84

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

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

85

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 the resultant increase of Xanthine and Hypoxanthine, both of which are more soluable and less likely to form crystals than uric acid

86

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

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

87

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

88

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

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

89

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

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

90

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

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

91

Monoclonal antibody used in the management of patients with renal allografts

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

92

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

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

93

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

94

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

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

95

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

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

96

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 the case of head injury, because of increased intracranial pressure

97

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

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

98

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

99

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 maternal circulation are opsonized by these antibodies, preventing the mother from producing anti–Rh antibodies

100

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

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

101

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

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

102

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

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

103

Used in the 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

104

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

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

105

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

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

106

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

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

107

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 HbF
▸ It also inhibits DNA synthesis by blocking the conversion of ribonucleotides to deoxyribonucleotides

108

Recombinately 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

109

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 significantly cheaper, although debatably equivalent, agent to tPA

110

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

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

111

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

TISSUE PLASMINOGEN ACTIVATOR (t–PA)
▸ Converts fibrin–bound plasminogen to plasmin, resulting in dissolution of thrombi

112

Orally administrated 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, X

113

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 H. pylori–associated Peptic Ulcer Disease

114

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

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

115

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

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

116

Prokinetic Agent used in the treatment of upper gastrointestinal dysfunction such as 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.

117

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

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

118

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

119

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

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

120

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

121

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

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

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

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

123

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

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

124

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

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

125

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

126

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

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

127

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

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

128

▸ 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

129

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

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

130

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

131

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

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

132

Non–sedating Antihistaminics used in the treatment of Allergy

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

133

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

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

134

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

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

135

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

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

136

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

137

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

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

138

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

139

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

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

140

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

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

141

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

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

142

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

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

143

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

DANAZOL
▸ Inhibits several P450 enzymes involved in gonadal steroid synthesis

144

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

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

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

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

146

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

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

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

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

148

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

FLUDROCORTISONE
▸ Used in conjunction with glucocorticoids in post–adrenalectomy therapy

149

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

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

150

A Synthetic Thyroid Hormone used in the treatment of Hypothyroidism as seen in Hashimoto's Thyroiditis, Myxedema, and in 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, used less frequently

151

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

152

Abortifacient steroid receptor antagonist known as the "Morning After" Pill

MIFEPRISTONE (RU486)
▸ Blocks the binding of Progesterone to cytoplasmic receptors, preventing successful implantation

153

Synthetic Progesterone Analog used in oral contraceptives and implantable contraceptive devices

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

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

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

155

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

156

Oral agent used in the treatment of Hyperthyroidism

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

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

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

This Insulin Secretagogue has 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 beta cells by binding to potassium channels

159

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

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

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

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

161

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, Insulin Glargine, has an even longer duration of action

162

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

ACYCLOVIR

163

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

ACYCLOVIR

164

▸ 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

AMANTADINE

165

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

AMANTADINE, RIMANTADINE

166

Longer half life than Amantadine with same action

RIMANTADINE

167

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

AMINOGLYCOSIDES

(GENTAMICIN, NEOMYCIN, AMIKACIN, TOBRAMYCIN, STREPTOMYCIN)

168

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

AMINOGLYCOSIDES

(GENTAMICIN, NEOMYCIN, AMIKACIN, TOBRAMYCIN, STREPTOMYCIN)

169

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

AMPHOTERICIN B

170

▸ 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)

AMPHOTERICIN B

171

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

AMPICILLIN

172

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

AMOXICILLIN

173

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

AZTREONAM

174

▸ Ineffective against GP or anaerobic bacteria
▸ Works synergistically with Aminoglycosides against GNR

AZTREONAM

175

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

BACITRACIN

176

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

BACITRACIN

177

▸ Extended–Spectrum Penicillins
▸ Useful against Pseudomonas and Enterobacter

CARBENICILLIN, PIPERACILLIN, TICARCILLIN

178

Can be used with Penicillinase Inhibitors and work synergistically with Aminoglycosides

CARBENICILLIN, PIPERACILLIN, TICARCILLIN

179

▸ Used for treatment of septic meningitis
▸ This Cephalosporin has good penetration into CNS

CEFTRIAXONE

180

▸ 3rd Generation Cephalosporin
▸ Coverage against Bacterial Meningitis – Strep pneumoniae, H. influenzae, Neisseria meningitides

CEFTRIAXONE

181

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

CHLORAMPHENICOL

182

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

CHLORAMPHENICOL

183

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

CHLORAMPHENICOL

184

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

CHLOROQUINE

185

▸ Kills parasites within erythrocytes (Schizonticidal)
▸ It disrupts hemoglobin breakdown, with the accumulation of heme, which is toxic to the organism

CHLOROQUINE

186

Administered with Penicillins to enhance their antimicrobial effects

CLINDAMYCIN

187

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

CLINDAMYCIN

188

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

DIDANOSINE (DDI)

189

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

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

190

NRTI that also inhibits Reverse Transcriptase of HBV

LAMIVUDINE (3TC)

191

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

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

192

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

MACROLIDES
▸ Erythromycin
▸ Azithromycin
▸ Clarithromycin

193

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

FLUOROQUINOLONES
▸ Ciprofloxacin
▸ Norfloxacin

194

Bactericidal inhibitor of DNA Gyrase, used for GNR, Neisseria

FLUOROQUINOLONES
▸ Ciprofloxacin
▸ Norfloxacin

195

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

FLUCONAZOLE

196

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

FLUCONAZOLE

197

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

FLUCONAZOLE

198

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

FOSCARNET

199

▸ 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

FOSCARNET

200

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

GANCICLOVIR

201

▸ 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

GANCICLOVIR

202

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

GRISEOFULVIN

203

Binds tubulin, interfering with MT function, inhibits mitosis

GRISEOFULVIN

204

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

IMIPENEM

205

▸ Used against GPC, GNR, anaerobes
▸ Metabolized by Renal Dihydropeptidase, which is blocked by coadministration of Cilastatin

IMIPENEM

206

Protease Inhibitors used in combined treatment regimens for HIV infection

Indinavir, Ritonavir, Saquinavir, Nelfinavir

207

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

Indinavir, Ritonavir, Saquinavir, Nelfinavir

208

▸ 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

ISONIAZID (INH)

209

▸ 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

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

210

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

IVERMECTIN

211

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

IVERMECTIN

212

▸ Used for the treatment of Mycotic Infections
▸ These agents inhibit hormone production and result in gynecomastia

AZOLES
▸ Ketoconazole
▸ Itraconazole
▸ Fluconazole

213

▸ 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

AZOLES
▸ Ketoconazole
▸ Itraconazole
▸ Fluconazole

214

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

MEBENDAZOLE

215

Functions by inhibiting microtubule synthesis and glucose uptake in helminthes

MEBENDAZOLE
▸ Related drugs such as Albendazole and Thiabendazole and alternatives

216

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

Methicillin, Nafcillin, Dicloxacillin

217

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

Methicillin, Nafcillin, Dicloxacillin

218

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

Metronidazole

219

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

Metronidazole

220

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

Neomycin

221

▸ 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

Neomycin

222

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

Nevirapine, Delavirdine, Efavirenz

223

▸ 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

Nevirapine, Delavirdine, Efavirenz

224

Trypanosomicidal drug used for the treatment of Chagas Disease

Nifurtimox

225

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

Nifurtimox

226

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

Nitrofurantoin

227

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

Nitrofurantoin

228

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

Nystatin

229

Disrupts fungal membrane permeability by binding to Ergosterol

Nystatin

230

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

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

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

Penicillins

232

▸ Mechanism is similar to Cephalosporins is nearly identical
▸ Major side effects: hypersensitivity with urticaria, and rarely, anaphylaxis leading to life–threatening asphyxiation

Penicillins

233

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

Polymixin B

234

▸ Acts as a cationic detergent that disrupts the membrane
▸ Systemic use causes neurotoxicity and acute tubular necrosis

Polymixin B

235

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

Praziquantel

236

Increases calcium permeability in the worm, resulting in paralysis

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

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

Pyrantel Pamoate

238

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

Pyrantel Pamoate

239

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

Quinine

240

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

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

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

Ribavirin

242

▸ 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

Ribavirin

243

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

Rifampin

244

▸ Inhibits DNA–Dependent RNA Polymerase
▸ Often used in a combined drug regimen for Mycobacterium tuberculosis because of rapid resistance if used alone

Rifampin

245

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

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

246

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

Streptogramins

247

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

Tetracycline

248

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

Tetracycline

249

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

Trimethoprin & Sulfamethoxazole
(TMP–SMX)

250

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

Trimethoprim, Sulfamethoxazole
(TMP–SMX)

251

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

Vancomycin

252

▸ Treatment of MRSA, Pseudomembranous Colitis due to C. diff
▸ SE can be limited by infusion over prolonged period and co–administration of antihistamines

Vancomycin

253

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

Zidovudine (ZDT)

254

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

Zidovudine (ZDT)

255

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

256

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

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

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

258

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

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

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

260

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

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

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

262

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

263

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

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

264

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

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

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

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

267

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

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

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

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

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

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

272

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

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

273

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

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

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

275

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

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

276

Q: Used for the treatment of acute iron toxicity.

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

277

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

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

278

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

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

279

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

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

280

Q: Used in the event of benzodiazepine overdose.

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

281

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

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

282

Q: Used to treat the symptoms of opioid overdose.

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

283

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

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

284

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

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

285

Q: Drugs that cause significant ototoxicity and nephrotoxicity.

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

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: Drugs that cause gynecomastia.

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

288

Q: Common drugs that inhibit hepatic P450 system.

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: Drugs that can cause massive hepatic necrosis.

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

290

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

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

291

Q: Drugs that inhibit microtubule function.

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: Drugs that cause a disulfram–like reaction.

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

293

Q: Drugs that cause cutaneous flushing on administration.

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: Bactericidal antibiotics.

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

295

Q: Drugs that induce the hepatic P450 system.

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

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

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: Drugs that cause photosensitivity.

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