BRS Pharm 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”.
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
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
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
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
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
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
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
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
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
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
12
Q
Used to prevent motion sickness and delivered by a transdermal patch
A
SCOPOLAMINE
▸ Competitive cholinergic antagonist with sedating and amnestic effects
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
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
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
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
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
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
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
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
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
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
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–
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
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
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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
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
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REPAGLINIDE
▸ Belongs to a class of drugs known as Meglitinides, which facilitate Insulin release from pancreatic beta cells by binding to potassium channels
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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).
