pharm step 1 Flashcards
(471 cards)
1
Q
Abciximab
A
Antiplatelet: monoclonal antibody to fibrin receptor (glycoprotein IIb/IIIa) on PLTs. Used to prevent clotting after coronary angioplasty
2
Q
Acarbose
A
Oral hypoglycemic: α-glucosidase inhibitor. Prevents oligosaccharide hydrolysis leading to less postprandial hyperglycemia. Tox: GI disturbances
3
Q
APAP
A
Antipyretic analgesic: CNS-active antipyretic, analgesic. Less toxic than aspirin but more dangerous in overdose (causes hepatic necrosis-antidote: acetylcysteine)
4
Q
Acetazolamide, Dorzolamide
A
Diuretic: carbonic anhydrase inhibitor. Causes
NaHCO3 diuresis and bicarbonate depletion at proximal tubule. Used in alkalosis, alkalinizing urine, glaucoma. Tox: metabolic acidosis. and therefore has self-limited action. Dorzolamide is a topical for glaucoma (decreases aqueous humor production)
5
Q
Acyclovir, valacyclovir, penciclovir, famciclovir
A
Antiviral: converted to dNTP analogs, inhibit DNA polymerase in HSV, VZV, EBV. Activated by viral thymidine kinase. Tox: tremor, delirium, crystallization in urinary tract
6
Q
Adenosine
A
Antiarrhythmic: “Class V”. IV only.
Hyperpolarizes AV node, blocking conduction for 10-15 sec. Used to dx, abolish nodal reentry arrhythmias.
7
Q
Albendazole, Mebendazole
A
Antihelminth: inhibit microtubule synthesis. Used for all roundworm infections.
8
Q
Allopurinol
A
Antigout: inhibitor of xanthine oxidase; prevents attacks during chronic gout and during chemotherapy for leukemia/ lymphoma
9
Q
Antiplatelet: monoclonal antibody to fibrin receptor (glycoprotein IIb/IIIa) on PLTs. Used to prevent clotting after coronary angioplasty
A
Abciximab
10
Q
Oral hypoglycemic: α-glucosidase inhibitor. Prevents oligosaccharide hydrolysis leading to less postprandial hyperglycemia. Tox: GI disturbances
A
Acarbose
11
Q
Antipyretic analgesic: CNS-active antipyretic, analgesic. Less toxic than aspirin but more dangerous in overdose (causes hepatic necrosis-antidote: acetylcysteine)
A
APAP
12
Q
Diuretic: carbonic anhydrase inhibitor. Causes
NaHCO3 diuresis and bicarbonate depletion at proximal tubule. Used in alkalosis, alkalinizing urine, glaucoma. Tox: metabolic acidosis. and therefore has self-limited action. Dorzolamide is a topical for glaucoma (decreases aqueous humor production)
A
Acetazolamide, Dorzolamide
13
Q
Antiviral: converted to dNTP analogs, inhibit DNA polymerase in HSV, VZV, EBV. Activated by viral thymidine kinase. Tox: tremor, delirium, crystallization in urinary tract
A
Acyclovir, valacyclovir, penciclovir, famciclovir
14
Q
Antiarrhythmic: “Class V”. IV only.
Hyperpolarizes AV node, blocking conduction for 10-15 sec. Used to dx, abolish nodal reentry arrhythmias.
A
Adenosine
15
Q
Antihelminth: inhibit microtubule synthesis. Used for all roundworm infections.
A
Albendazole, mebendazole
16
Q
Antigout: inhibitor of xanthine oxidase; prevents attacks during chronic gout and during chemotherapy for leukemia/ lymphoma
A
Allopurinol
17
Q
Albuterol, terbutaline
A
β2-agonists for asthma. Acute attacks only. Tox: tremor, arrhythmia.
18
Q
Alprazolam, lorazepam
A
Benzodiazepine: intermediate duration of action. Used in anxiety states, selectivity for panic attacks and phobias. Tox: psychologic and physical dependence, additive effects with other CNS depressants
19
Q
Amantadine, rimantadine
A
Antiviral: prevents uncoating of influenza A inside host cells. Reduces duration of flu symptoms. Amantadine also causes release of dopamine for Parkinson’s. Tox: ataxia, dysphasia.
20
Q
Amiodarone
A
Antiarrhythmic: action in all 4 Classes. Used for life-threatening atrial and ventricular arrhythmias. Tox: pulmonary fibrosis, hepatoxicity, thyroid dysfunction
21
Q
Amitriptyline, nortriptyline, desipramine, imipramine
A
TCA: blocks reuptake of NE and 5-HT. Tox: antimuscarinic (atropine-like), anti-α (orthostatic hypotension), sedation, overdose (seizures, coma, QRS widening). Additive effects with other CNS depressants. Use bicarb in toxicity.
22
Q
Amoxicillin, ampicillin
A
Penicillin (beta-lactam): better coverage than PCN. Amoxicillin is oral pills. Can be used for almost all mild infections. Penicillinase- susceptible unless given w/ inhibitor. Tox: penicillin allergy
23
Q
Amphetamine
A
Indirect sympathomimetic: releases catecholamine store. CNS stimulant action. Used for narcolepsy, obesity, ADHD. Tox: psychosis, HTN, MI, seizures
24
Q
Amphotericin B
A
Antifungal: 1st line for most systemic mycoses. Emulsifies fungal cell membrane by binding ergosterol. Tox: “shake and bake,” nephrotoxicity. Must be given intrathecally for meningitis. Nystatin is similar and used topically. Flucytosine is used w/ amphotericin to inhibit DNA/RNA synthesis.
25
β2-agonists for asthma. Acute attacks only. Tox: tremor, arrhythmia.
Albuterol, terbutaline
26
Benzodiazepine: intermediate duration of action. Used in anxiety states, selectivity for panic attacks and phobias. Tox: psychologic and physical dependence, additive effects with other CNS depressants
Alprazolam, lorazepam
27
Antiviral: prevents uncoating of influenza A inside host cells. Reduces duration of flu symptoms. Amantadine also causes release of dopamine for Parkinson’s. Tox: ataxia, dysphasia.
Amantadine, rimantadine
28
Antiarrhythmic: action in all 4 Classes. Used for life-threatening atrial and ventricular arrhythmias. Tox: pulmonary fibrosis, hepatoxicity, thyroid dysfunction
Amiodarone
29
TCA: blocks reuptake of NE and 5-HT. Tox: antimuscarinic (atropine-like), anti-α (orthostatic hypotension), sedation, overdose (seizures, coma, QRS widening). Additive effects with other CNS depressants. Use bicarb in toxicity.
Amitriptyline, nortriptyline, desipramine, imipramine
30
Penicillin (beta-lactam): better coverage than PCN. Amoxicillin is oral pills. Can be used for almost all mild infections. Penicillinase- susceptible unless given w/ inhibitor. Tox: penicillin allergy
Amoxicillin, ampicillin
31
Indirect sympathomimetic: releases catecholamine store. CNS stimulant action. Used for narcolepsy, obesity, ADHD. Tox: psychosis, HTN, MI, seizures
Amphetamine
32
Antifungal: 1st line for most systemic mycoses. Emulsifies fungal cell membrane by binding ergosterol. Tox: “shake and bake,” nephrotoxicity. Must be given intrathecally for meningitis. Nystatin is similar and used topically. Flucytosine is used w/ amphotericin to inhibit DNA/RNA synthesis.
Amphotericin B
33
Antistreplase (APSAC)
Thrombolytic: longer acting in body than other thrombolytics (rt-PA, streptokinase, urokinase). Tox: bleeding, allergy to streptococcal protein
34
ASA
NSAID prototype: inhibits cyclooxygenase (COX) I and II irreversibly. Potent antiplatelet agent as well as antipyretic analgesic anti- inflammatory drug. In overdose, alkalinize urine and dialyze
35
Atenolol
β1-selective blocker: low lipid solubility, less CNS effect; used for HTN. Mnemonic for β1- selective blockers: their names start with A through M. (except labetalol)
36
Atropine
Antimuscarinic: lipid soluble, CNS effects. Tox: “blind as a bat, dry as a bone, hot as a hare, mad as a hatter, red as a beet," urinary retention, mydriasis. Use physostigmine in toxicity. Blocks “SLUD”: salivation, lacrimation, urination, defecation
37
Azathioprine
Immunosuppressant: similar to 6-MP but for kidney transplant. Tox: myelosuppression, xanthine oxidase-dependent
38
Aztreonam
Monocyclic β-lactam. Penicillinase-resistant. Used only against GN bugs, especially nasty GNRs. Not a cross-allergen w/ PCN, can be used in CKD patients (unlike aminoglycosides)
39
Baclofen
GABA-analog spasmolytic: activates GABAB receptors in the spinal cord.
40
Beclomethasone
Inhaled corticosteroid for chronic asthma.
41
Thrombolytic: longer acting in body than other thrombolytics (rt-PA, streptokinase, urokinase). Tox: bleeding, allergy to streptococcal protein
Anistreplase (APSAC)
42
NSAID prototype: inhibits cyclooxygenase (COX) I and II irreversibly. Potent antiplatelet agent as well as antipyretic analgesic anti- inflammatory drug. In overdose, alkalinize urine and dialyze
ASA
43
β1-selective blocker: low lipid solubility, less CNS effect; used for HTN. Mnemonic for β1- selective blockers: their names start with A through M. (except labetalol)
Atenolol
44
Antimuscarinic: lipid soluble, CNS effects. Tox: “blind as a bat, dry as a bone, hot as a hare, mad as a hatter, red as a beet," urinary retention, mydriasis. Use physostigmine in toxicity. Blocks “SLUD”: salivation, lacrimation, urination, defecation
Atropine
45
Immunosuppressant: similar to 6-MP but for kidney transplant. Tox: myelosuppression, xanthine oxidase-dependent
Azathioprine
46
Monocyclic β-lactam. Penicillinase-resistant. Used only against GN bugs, especially nasty GNRs. Not a cross-allergen w/ PCN, can be used in CKD patients (unlike aminoglycosides)
Aztreonam
47
GABA-analog spasmolytic: activates GABAB receptors in the spinal cord.
Baclofen
48
Inhaled corticosteroid for chronic asthma.
Beclomethasone
49
Benztropine
Central antimuscarinic for Parkinsonian tremor/rigidity
50
Bethanechol
Muscarinic agonist: choline ester with good resistance to cholinesterase. Used for postop or neurogenic ileus or urinary retention.
51
Bismuth, sucralafate
Antiulcer: protect ulcer base and hasten recovery.
52
Bleomycin
Antineoplastic: causes free radical DNA damage. Used in testicular ca, lymphomas (ABVD). Tox: pulmonary fibrosis.
53
Bromocriptine, pramipexole, ropinirole
Ergot alkaloid: dopamine agonist in CNS; inhibits prolactin. Used in Parkinson’s hyperprolactinemia. Tox: CNS, dyskinesias, hypotension
54
Bupivacaine, lidocaine, tetracaine, procaine, cocaine
Local anesthetics: block Na+ channels. 2 I’s in name: amide. 1 I in name: ester. Does not penetrate infected tissue well. Causes loss of sensation in this order: pain, temperature, touch, pressure. Tox: CNS excitation, severe myocardial toxicity (bupivicaine), arrhythmia (cocaine).
55
Bupropion
Heterocyclic antidepressant: MOA unknown. Also used for smoking cessation. Tox: stimulant-like, seizure in bulimics.
56
Buspirone
Anxiolytic: atypical drug that interacts with 5HT1A receptors; slow onset. Minimal potentiation of CNS depressants including ethanol; negligible abuse liability
57
Central antimuscarinic for Parkinsonian tremor/rigidity
Benztropine
58
Muscarinic agonist: choline ester with good resistance to cholinesterase. Used for postop or neurogenic ileus or urinary retention.
Bethanechol
59
Antiulcer: protect ulcer base and hasten recovery.
Bismuth, sucralafate
60
Ergot alkaloid: dopamine agonist in CNS; inhibits prolactin. Used in Parkinson’s hyperprolactinemia. Tox: CNS, dyskinesias, hypotension
Bromocriptine, pramipexole, ropinirole
61
Local anesthetics: block Na+ channels. 2 I’s in name: amide. 1 I in name: ester. Does not penetrate infected tissue well. Causes loss of sensation in this order: pain, temperature, touch, pressure. Tox: CNS excitation, severe myocardial toxicity (bupivicaine), arrhythmia (cocaine).
Bupivacaine, lidocaine, tetracaine, procaine, cocaine
62
Heterocyclic antidepressant: MOA unknown. Also used for smoking cessation. Tox: stimulant-like, seizure in bulimics.
Bupropion
63
Anxiolytic: atypical drug that interacts with 5HT1A receptors; slow onset. Minimal potentiation of CNS depressants including ethanol; negligible abuse liability
Buspirone
64
Antineoplastic: causes free radical DNA damage. Used in testicular ca, lymphomas (ABVD). Tox: pulmonary fibrosis.
Bleomycin
65
Busulfan
Antineoplastic: DNA alkylator. Used in CML. Tox: pulmonary fibrosis.
66
Captopril
ACE inhibitor: used in HTN, diabetic renal disease, and CHF. Tox: cough, angioedema (both due to increased bradykinin) proteinuria, teratogen to fetal kidneys, hyperkalemia. In CKD, the action of A-II may be all that is preserving GFR.
67
Carbachol, pilocarpine
Nonselective muscarinic and nicotinic agonist: choline ester with good resistance to cholinesterase; used for glaucoma (not 1st-line)
68
Carbamazepine
Anticonvulsant: 1st line for tonic-clonic and trigeminal neuralgia, also used ( phenytoin, valproate) for partial seizures. Same MOA as phenytoin (Na+ channel blocker). Tox: diplopia, ataxia, agranulocytosis, aplastic anemia, hepatotoxicity, teratogen, induces P450
69
Caspofungin
Antifungal: disrupts fungal cell wall synthesis.
70
Cefazolin, cephalexin
1st-gen cephalosporin: bactericidal β- lactamase-resistant β-lactams. Used for GPCs, weak activity against GNRs. Tox: potential allergy
71
Cefuroxime, cefoxitin, cefotetan
2nd-gen cephalosporin. Used for GPCs, H. flu, Klebsiella, in sinusitis or otitis.
72
Ceftriaxone, ceftaz, ceftiz
3rd-gen cephalosporin. Used in nasty GN sepsis and meningitis (also covers Pneumococcus).
73
Antineoplastic: DNA alkylator. Used in CML. Tox: pulmonary fibrosis.
Busulfan
74
ACE inhibitor: used in HTN, diabetic renal disease, and CHF. Tox: cough, angioedema (both due to increased bradykinin) proteinuria, teratogen to fetal kidneys, hyperkalemia. In CKD, the action of A-II may be all that is preserving GFR.
Captopril
75
Nonselective muscarinic and nicotinic agonist: choline ester with good resistance to cholinesterase; used for glaucoma (not 1st-line)
Carbachol, pilocarpine
76
Anticonvulsant: 1st line for tonic-clonic and trigeminal neuralgia, also used ( phenytoin, valproate) for partial seizures. Same MOA as phenytoin (Na+ channel blocker). Tox: diplopia, ataxia, agranulocytosis, aplastic anemia, hepatotoxicity, teratogen, induces P450
Carbamazepine
77
Antifungal: disrupts fungal cell wall synthesis.
Caspofungin
78
1st-gen cephalosporin: bactericidal β- lactamase-resistant β-lactams. Used for GPCs, weak activity against GNRs. Tox: potential allergy
Cefazolin, cephalexin
79
2nd-gen cephalosporin. Used for GPCs, H. flu, Klebsiella, in sinusitis or otitis.
Cefuroxime, cefoxitin, cefotetan
80
3rd-gen cephalosporin. Used in nasty GN sepsis and meningitis (also covers Pneumococcus).
Ceftriaxone, ceftaz, ceftiz
81
Cefepime
4th-gen cephalosporin: developed to treat Pseudomonas.
82
Celecoxib, rofecoxib
First COX-II-selective NSAIDs. Reduced GI toxicity, increased thrombosis
83
Chloramphenicol
Antibiotic: inhibits peptidyl transferase at 50S subunit. Can be used for almost any bugs, but is rarely used due to side effects. Tox: reversible myelosuppression, aplastic anemia, “gray baby” syndrome due to inhibition of UDP-glucuronyl transferase
84
Chloroquine, mefloquine, primaquine
Antimalarial: kill blood forms of Plasmodium. Chloroquine resistance is widespread. Primaquine is active against liver forms. Tox: GI distress, rash, G6PD oxidant effect
85
Cholestyramine, colestipol
Antilipemic: bind bile acids to prevent reabsorption; body converts more cholesterol to bile salts to compensate. Tox: constipation, bloating, terrible taste
86
Cimetidine
H2 blocker prototype: used in GERD, ulcers. Tox: inhibits hepatic drug metabolism; antiandrogen effects. Analogs w/ neither toxicity:: ranitidine, famotidine, etc
87
Ciprofloxacin, "-floxacin"s
Fluoroquinolone: bactericidal inhibitor of topoisomerase. Used against most GNRs in UTIs, bacterial diarrhea. Tox: GI distress, cartilage damage in tendons causing tendonitis, tendon rupture. Avoid in children and pregnant women.
88
Cisplatin
Antineoplastic: DNA alkylator. Used for testicular, bladder ca. Tox: kidney, acoustic nerve. Carboplatin is similar.
89
4th-gen cephalosporin: developed to treat Pseudomonas.
Cefepime
90
First COX-II-selective NSAIDs. Reduced GI toxicity, increased thrombosis
Celecoxib, rofecoxib
91
Antibiotic: inhibits peptidyl transferase at 50S subunit. Can be used for almost any bugs, but is rarely used due to side effects. Tox: reversible myelosuppression, aplastic anemia, “gray baby” syndrome due to inhibition of UDP-glucuronyl transferase
Chloramphenicol
92
Antimalarial: kill blood forms of Plasmodium. Chloroquine resistance is widespread. Primaquine is active against liver forms. Tox: GI distress, rash, G6PD oxidant effect
Chloroquine, mefloquine, primaquine
93
Antilipemic: bind bile acids to prevent reabsorption; body converts more cholesterol to bile salts to compensate. Tox: constipation, bloating, terrible taste
Cholestyramine, colestipol
94
H2 blocker prototype: used in GERD, ulcers. Tox: inhibits hepatic drug metabolism; antiandrogen effects. Analogs w/ neither toxicity:: ranitidine, famotidine, etc
Cimetidine
95
Fluoroquinolone: bactericidal inhibitor of topoisomerase. Used against most GNRs in UTIs, bacterial diarrhea. Tox: GI distress, cartilage damage in tendons causing tendonitis, tendon rupture. Avoid in children and pregnant women.
Ciprofloxacin, "-floxacin"s
96
Antineoplastic: DNA alkylator. Used for testicular, bladder ca. Tox: kidney, acoustic nerve. Carboplatin is similar.
Cisplatin
97
Antineoplastic: DNA alkylator. Used for testicular, bladder ca. Tox: kidney, acoustic nerve. Carboplatin is similar.
Cisplatin
98
Clindamycin
Antibiotic: bacteriostatic, inhibits formation of initiation complex at the 50S subunit. Used against anaerobic pneumonia and GPCs. Tox: GI distress, pseudomembranous colitis. Linezolid is similar but used for MRSA, VRE.
99
Clomiphene
Estrogen partial agonist at pituitary: causes release of FSH and LH, inducing ovulation. Used to treat infertility. Tox: hot flashes, ovary-megaly, twins or triplets.
100
Clonidine
α2 agonist: acts centrally to reduce SNS outflow, lowers BP. Tox: rebound HTN, sedation, dry mouth. Methyldopa is similar but causes positive Coombs’.
101
Clozapine, olanzapine, risperidone
Atypical antipsychotic: low affnity for dopamine D2 receptors, higher for D4 and 5-HT2A receptors. Used for schizophrenia; olanzapine used for OCD, anxiety, etc. Tox: less EPS, anticholinergic effects than neuroleptics. Clozapine requires weekly WBC for r/o agranulocytosis, causes weight gain
102
Cocaine
Indirect sympathomimetic: blocks catecholamine reuptake. Local anesthetic (ester type). Used for nasal surgery. Marked CNS stimulation, euphoria; high abuse liability. Tox: stroke, psychosis, arrhythmias, seizures
103
Colchicine
Microtubule assembly inhibitor: “freezes” WBCs in gouty joints. Tox: GI, hepatic, renal
104
Cromolyn
Anti-asthma: mast cell stabilizer. 3rd line agent for prophylaxis.
105
Cyanide
Toxin: poisons oxidative phosphorylation and creates metHb. Use nitrites in toxicity
106
Antibiotic: bacteriostatic, inhibits formation of initiation complex at the 50S subunit. Used against anaerobic pneumonia and GPCs. Tox: GI distress, pseudomembranous colitis. Linezolid is similar but used for MRSA, VRE.
Clindamycin
107
Estrogen partial agonist at pituitary: causes release of FSH and LH, inducing ovulation. Used to treat infertility. Tox: hot flashes, ovary-megaly, twins or triplets.
Clomiphene
108
α2 agonist: acts centrally to reduce SNS outflow, lowers BP. Tox: rebound HTN, sedation, dry mouth. Methyldopa is similar but causes positive Coombs’.
Clonidine
109
Atypical antipsychotic: low affnity for dopamine D2 receptors, higher for D4 and 5-HT2A receptors. Used for schizophrenia; olanzapine used for OCD, anxiety, etc. Tox: less EPS, anticholinergic effects than neuroleptics. Clozapine requires weekly WBC for r/o agranulocytosis, causes weight gain
Clozapine, olanzapine, risperidone
110
Indirect sympathomimetic: blocks catecholamine reuptake. Local anesthetic (ester type). Used for nasal surgery. Marked CNS stimulation, euphoria; high abuse liability. Tox: stroke, psychosis, arrhythmias, seizures
Cocaine
111
Microtubule assembly inhibitor: “freezes” WBCs in gouty joints. Tox: GI, hepatic, renal
Colchicine
112
Anti-asthma: mast cell stabilizer. 3rd line agent for prophylaxis.
Cromolyn
113
Toxin: poisons oxidative phosphorylation and creates metHb. Use nitrites in toxicity
Cyanide
114
Cyclophosphamide, ifosfamide
Antineoplastic, immunosuppressive: DNA alkylating agent. Used in HL, breast ca. Tox: Hemorrhagic cystitis (prevent w/ mesna), myelosuppression
115
Cyclosporine
Immunosuppressant: inhibits calcineurin, and thereby IL-2. Used in transplant immunosuppression. Tox: nephrotoxicity (dose-limiting), infections. Tacrolimus is nearly identical
116
Cytarabine
Antineoplastic: DNA polymerase inhibitor. Used in AML. Tox: leukopenia.
117
Dactinomycin
Antineoplastic: intercalates in DNA. Used in Wilms’, Ewing’s, rhabdomyosarcoma (kids’ tumors)
118
Dantrolene
Blocker of Ca2+ release from sarcoplasmic reticulum of skeletal muscle. Used for malignant hyperthermia, muscle spasm, malignant neuroleptic syndrome, and serotonin syndrome.
119
Daunorubicin
Like doxorubicin but only used for AML
120
Deferoxamine
Chelator: chelates Fe very avidly, aluminum less so
121
Antineoplastic, immunosuppressive: DNA alkylating agent. Used in HL, breast ca. Tox: Hemorrhagic cystitis (prevent w/ mesna), myelosuppression
Cyclophosphamide, ifosfamide
122
Immunosuppressant: inhibits calcineurin, and thereby IL-2. Used in transplant immunosuppression. Tox: nephrotoxicity (dose-limiting), infections. Tacrolimus is nearly identical
Cyclosporine
123
Antineoplastic: DNA polymerase inhibitor. Used in AML. Tox: leukopenia.
Cytarabine
124
EPO: renal-failure anemia. G-CSF/GM-CSF: recover bone marrow.
IFN-α: HBV or HCV, HHV-8.
IFN-β": MS.
IFN-ɣ: CGD.
Cytokines
125
Antineoplastic: intercalates in DNA. Used in Wilms’, Ewing’s, rhabdomyosarcoma (kids’ tumors)
Dactinomycin
126
Blocker of Ca2+ release from sarcoplasmic reticulum of skeletal muscle. Used for malignant hyperthermia, muscle spasm, malignant neuroleptic syndrome, and serotonin syndrome.
Dantrolene
127
Like doxorubicin but only used for AML
Daunorubicin
128
Chelator: chelates Fe very avidly, aluminum less so
Deferoxamine
129
Desmopressin
ADH analog: synthetic peptide used for pituitary diabetes insipidus, vWD.
130
Dexamethasone
Glucocorticoid: very potent, long-acting; no mineralocorticoid activity
131
Diazepam
Benzodiazepine: binds to BDZ receptors at the GABAA receptor, increasing frequency of channel opening. Uses: anxiety, EtOH detox, muscle spasms, status epilepticus. Tox: psychologic and physical dependence, additive effects with other CNS depressants
132
Digoxin
Cardiac glycoside prototype: positive inotropic drug for CHF. Used in CHF, a-fib (decreases AV nodal conduction). Half-life 40h. Renal excretion. Can cause long PR, short QT, ST scooping, inverted T. Tox: N/V, diarrhea. Toxicity exacerbated by hypokalemia, renal failure, quinidine. Anti-dig Fab available.
133
Dimercaprol
Chelator (British AntiLewisite): used for As, Pb, Hg poisoning. 1st line for Pb
134
Diphenhydramine, chlorpheniramine
Antihistamine H1 blocker prototype: used in hayfever, motion sickness, sleep aid. Tox: antimuscarinic, anti-α, sedative
135
Dobutamine
β1 agonist: pure inotrope for ICU care.
136
Donepezil, tacrine
Antialzheimer: centrally-active cholinesterase inhibitor to slow progression of symptoms
137
ADH analog: synthetic peptide used for pituitary diabetes insipidus, vWD.
Desmopressin
138
Glucocorticoid: very potent, long-acting; no mineralocorticoid activity
Dexamethasone
139
Benzodiazepine: binds to BDZ receptors at the GABAA receptor, increasing frequency of channel opening. Uses: anxiety, EtOH detox, muscle spasms, status epilepticus. Tox: psychologic and physical dependence, additive effects with other CNS depressants
Diazepam
140
Cardiac glycoside prototype: positive inotropic drug for CHF. Used in CHF, a-fib (decreases AV nodal conduction). Half-life 40h. Renal excretion. Can cause long PR, short QT, ST scooping, inverted T. Tox: N/V, diarrhea. Toxicity exacerbated by hypokalemia, renal failure, quinidine. Anti-dig Fab available.
Digoxin
141
Chelator (British AntiLewisite): used for As, Pb, Hg poisoning. 1st line for Pb
Dimercaprol
142
Antihistamine H1 blocker prototype: used in hayfever, motion sickness, sleep aid. Tox: antimuscarinic, anti-α, sedative
Diphenhydratmine, chlorpheniramine
143
β1 agonist: pure inotrope for ICU care.
Dobutamine
144
Antialzheimer: centrally-active cholinesterase inhibitor to slow progression of symptoms
Donepezil, tacrine
145
Antialzheimer: centrally-active cholinesterase inhibitor to slow progression of symptoms
Donepezil, tacrine
146
Dopamine
Neurotransmitter and agonist drug at dopamine receptors: pressor for shock and to increase renal blood flow
147
Doxorubicin
Antineoplastic: anthracycline drug (cell cycle- nonspecific); intercalates between base pairs to disrupt DNA functions and forms cytotoxic free radicals. Used in breast, most solid tumors, HL (ABVD regimen) Tox: cardiotoxicity, myelosuppression
148
Edetate (EDTA)
Chelating agent: 1st line for Pb poisoning. Tox: renal tubular necrosis
149
Ephedrine
Indirect sympathomimetic: like amphetamine but less CNS stimulation. Used for nasal decongestion, urinary incontinence
150
Epinephrine
Agonist at all α and β receptors. Used in anaphylaxis, asthma, ICU hypotension, vasoconstriction w/ local anesthesia.
151
Erythromycin, azithromycin, clarithromycin
Macrolide: bacteriostatic, inhibits translocation at the 50S subunit. Used mostly for atypical pneumonias and Chlamydia UTI. Tox: cholestatic hepatitis, erythromycin inhibits P450 to increase warfarin, theophylline, cyclosporine concentrations.
152
Etanercept
Soluble TNF receptor: used in RA, psoriasis.
153
Ethacrynic acid
Loop diuretic: same as furosemide in action and toxicity w/o gout or allergy.
154
Neurotransmitter and agonist drug at dopamine receptors: pressor for shock and to increase renal blood flow
Dopamine
155
Antineoplastic: anthracycline drug (cell cycle- nonspecific); intercalates between base pairs to disrupt DNA functions and forms cytotoxic free radicals. Used in breast, most solid tumors, HL (ABVD regimen) Tox: cardiotoxicity, myelosuppression
Doxorubicin
156
Chelating agent: 1st line for Pb poisoning. Tox: renal tubular necrosis
Edetate (EDTA)
157
Indirect sympathomimetic: like amphetamine but less CNS stimulation. Used for nasal decongestion, urinary incontinence
Ephedrine
158
Agonist at all α and β receptors. Used in anaphylaxis, asthma, ICU hypotension, vasoconstriction w/ local anesthesia.
Epinephrine
159
Macrolide: bacteriostatic, inhibits translocation at the 50S subunit. Used mostly for atypical pneumonias and Chlamydia UTI. Tox: cholestatic hepatitis, erythromycin inhibits P450 to increase warfarin, theophylline, cyclosporine concentrations.
Erythromycin, azithromycin, clarithromycin
160
Soluble TNF receptor: used in RA, psoriasis.
Etanercept
161
Loop diuretic: same as furosemide in action and toxicity w/o gout or allergy.
Ethacrynic acid
162
Ethanol
Sedative-hypnotic: increases flow through GABAA channels. Metabolized by alcohol dehydrogenase to acetaldehyde, then by aldehyde dehydrogenase to acetate. Disulfiram inhibits aldehyde dehydrogenase, causing accumulation of acetaldehyde. Consumes NAD + and produces NADH. Zero-order elimination kinetics, chronically induces its own metabolism.
163
Ethosuximide
Anticonvulsant: 1st line for absence. Blocks thalamic T-type Ca2+ channels. Tox: GI distress, lethargy, Stevens-Johnson
164
Etidronate, pamidronate, alendronate
Bisphosphonates: reduce resorption of bone by inserting into hydroxyapatite. Used in Paget’s disease, osteoporosis, PTH-rP secretion. Tox: severe esophageal ulceration
165
Etoposide
Antineoplastic: inhibits topoisomerase only during G2. Used in small cell carcinomas. Tox: myelosuppression
166
Fexofenadine, loratadine, desloratadine
2nd generation antihistamine; does not enter CNS, little or no sedation
167
Finasteride
Steroid inhibitor of 5α-reductase: inhibits synthesis of DHT, the active androgen in prostate. Used in BPH.
168
Flecainide, encainide
Class IC antiarrhythmics. Used for severe, refractory ventricular arrhythmias. Tox: propafenone arrhythmogenic, contraindicated post-MI
169
Fluconazole, itraconazole
Antifungal: inhibits fungal and host P450. Used for more severe infxns than ketoconazole: Cryptococcal meningitis, Candida sepsis. No antiandrogenic effects.
170
Sedative-hypnotic: increases flow through GABAA channels. Metabolized by alcohol dehydrogenase to acetaldehyde, then by aldehyde dehydrogenase to acetate. Disulfiram inhibits aldehyde dehydrogenase, causing accumulation of acetaldehyde. Consumes NAD + and produces NADH. Zero-order elimination kinetics, chronically induces its own metabolism.
Ethanol
171
Anticonvulsant: 1st line for absence. Blocks thalamic T-type Ca2+ channels. Tox: GI distress, lethargy, Stevens-Johnson
Ethosuximide
172
Bisphosphonates: reduce resorption of bone by inserting into hydroxyapatite. Used in Paget’s disease, osteoporosis, PTH-rP secretion. Tox: severe esophageal ulceration
Etidronate, pamidronate, alendronate
173
Antineoplastic: inhibits topoisomerase only during G2. Used in small cell carcinomas. Tox: myelosuppression
Etoposide
174
2nd generation antihistamine; does not enter CNS, little or no sedation
Fexofenadine, loratadine, desloratadine
175
Steroid inhibitor of 5α-reductase: inhibits synthesis of DHT, the active androgen in prostate. Used in BPH.
Finasteride
176
Class IC antiarrhythmics. Used for severe, refractory ventricular arrhythmias. Tox: propafenone arrhythmogenic, contraindicated post-MI
Flecainide, encanide
177
Antifungal: inhibits fungal and host P450. Used for more severe infxns than ketoconazole: Cryptococcal meningitis, Candida sepsis. No antiandrogenic effects.
Fluconazole, itraconazole
178
Amitriptyline, nortriptyline, desipramine, imipramine
TCA: blocks reuptake of NE and 5-HT. Tox: antimuscarinic (atropine-like), anti-α (orthostatic hypotension), sedation, overdose (seizures, coma, QRS widening). Additive effects with other CNS depressants. Use bicarb in toxicity.
179
TCA: blocks reuptake of NE and 5-HT. Tox: antimuscarinic (atropine-like), anti-α (orthostatic hypotension), sedation, overdose (seizures, coma, QRS widening). Additive effects with other CNS depressants. Use bicarb in toxicity.
Amitriptyline, nortriptyline, desipramine, imipramine
180
Antimuscarinic: lipid soluble, CNS effects. Tox: “blind as a bat, dry as a bone, hot as a hare, mad as a hatter, red as a beet," urinary retention, mydriasis. Use physostigmine in toxicity. Blocks “SLUD”: salivation, lacrimation, urination, defecation
Atropine
181
Chloramphenicol
Antibiotic: inhibits peptidyl transferase at 50S subunit. Can be used for almost any bugs, but is rarely used due to side effects. Tox: reversible myelosuppression, aplastic anemia, “gray baby” syndrome due to inhibition of UDP-glucuronyl transferase
182
Chloroquine, mefloquine, primaquine
Antimalarial: kill blood forms of Plasmodium. Chloroquine resistance is widespread. Primaquine is active against liver forms. Tox: GI distress, rash, G6PD oxidant effect
183
Cimetidine
H2 blocker prototype: used in GERD, ulcers. Tox: inhibits hepatic drug metabolism; antiandrogen effects. Analogs w/ neither toxicity:: ranitidine, famotidine, etc
184
Antibiotic: inhibits peptidyl transferase at 50S subunit. Can be used for almost any bugs, but is rarely used due to side effects. Tox: reversible myelosuppression, aplastic anemia, “gray baby” syndrome due to inhibition of UDP-glucuronyl transferase
Chloramphenicol
185
Antimalarial: kill blood forms of Plasmodium. Chloroquine resistance is widespread. Primaquine is active against liver forms. Tox: GI distress, rash, G6PD oxidant effect
Chloroquine, mefloquine, primaquine
186
H2 blocker prototype: used in GERD, ulcers. Tox: inhibits hepatic drug metabolism; antiandrogen effects. Analogs w/ neither toxicity:: ranitidine, famotidine, etc
Cimetidine
187
Clozapine, olanzapine, risperidone
Atypical antipsychotic: low affnity for dopamine D2 receptors, higher for D4 and 5-HT2A receptors. Used for schizophrenia; olanzapine used for OCD, anxiety, etc. Tox: less EPS, anticholinergic effects than neuroleptics. Clozapine requires weekly WBC for r/o agranulocytosis, causes weight gain
188
Atypical antipsychotic: low affnity for dopamine D2 receptors, higher for D4 and 5-HT2A receptors. Used for schizophrenia; olanzapine used for OCD, anxiety, etc. Tox: less EPS, anticholinergic effects than neuroleptics. Clozapine requires weekly WBC for r/o agranulocytosis, causes weight gain
Clozapine, olanzapine, risperidone
189
Diazepam
Benzodiazepine: binds to BDZ receptors at the GABAA receptor, increasing frequency of channel opening. Uses: anxiety, EtOH detox, muscle spasms, status epilepticus. Tox: psychologic and physical dependence, additive effects with other CNS depressants
190
Benzodiazepine: binds to BDZ receptors at the GABAA receptor, increasing frequency of channel opening. Uses: anxiety, EtOH detox, muscle spasms, status epilepticus. Tox: psychologic and physical dependence, additive effects with other CNS depressants
Diazepam
191
Fluconazole, itraconazole
Antifungal: inhibits fungal and host P450. Used for more severe infxns than ketoconazole: Cryptococcal meningitis, Candida sepsis. No antiandrogenic effects.
192
Antifungal: inhibits fungal and host P450. Used for more severe infxns than ketoconazole: Cryptococcal meningitis, Candida sepsis. No antiandrogenic effects.
Fluconazole, itraconazole
193
Flucortisone
Synthetic corticosteroid: high mineralocorticoid and moderate glucocorticoid activity; long duration of action
194
Flumazenil
Benzodiazepine antagonist: used to reverse CNS depressant effects of benzos in overdose or in anesthesia
195
5-Fluorouracil
Antineoplastic: pyrimidine antimetabolite (S phase) that decreases dTMP. Used mainly for colon ca or superficial tumors. Tox: myelosuppression not rescuable w/ leucovorin
196
Fluoxetine, paroxetine, sertraline, citalopram
SSRI antidepressant. Also used for OCD. Takes effect in 2-3 weeks. Tox: less antimuscarinic, cardiotoxic; more GI distress and sexual dysfunction. Causes serotonin syndrome if used w/ MAOI. Fluoxetine inhibits P450.
197
Flutamide
Androgen receptor antagonist: nonsteroid that blocks DHT. Used in prostate ca.
198
Furosemide
Loop diuretic: blocks Na+/K+/2Cl- transporter, preventing urine concentration. Used for edema states, hypercalcemia. Can be used in severe renal disease. Tox: hypokalemia, allergy to sulfa, ototoxicity, hypovolemia, gout, hypocalcemia.
199
Gabapentin
Anticonvulsant and analgesic: increases CNS GABA. Used for general and partial seizures and peripheral neuropathy. Tox: sedation, ataxia.
200
Ganciclovir, foscarnet
Antiviral: GTP analog that requires activation by thymidine kinase. Used for CMV. Tox: neutropenia. Foscarnet does not require activation.
201
Synthetic corticosteroid: high mineralocorticoid and moderate glucocorticoid activity; long duration of action
Fludrocortisone
202
Benzodiazepine antagonist: used to reverse CNS depressant effects of benzos in overdose or in anesthesia
Flumazenil
203
Antineoplastic: pyrimidine antimetabolite (S phase) that decreases dTMP. Used mainly for colon ca or superficial tumors. Tox: myelosuppression not rescuable w/ leucovorin
5-Fluorouracil
204
SSRI antidepressant. Also used for OCD. Takes effect in 2-3 weeks. Tox: less antimuscarinic, cardiotoxic; more GI distress and sexual dysfunction. Causes serotonin syndrome if used w/ MAOI. Fluoxetine inhibits P450.
Fluoxetine, paroxetine, sertraline, citalopram
205
Androgen receptor antagonist: nonsteroid that blocks DHT. Used in prostate ca.
Flutamide
206
Loop diuretic: blocks Na+/K+/2Cl- transporter, preventing urine concentration. Used for edema states, hypercalcemia. Can be used in severe renal disease. Tox: hypokalemia, allergy to sulfa, ototoxicity, hypovolemia, gout, hypocalcemia.
Furosemide
207
Anticonvulsant and analgesic: increases CNS GABA. Used for general and partial seizures and peripheral neuropathy. Tox: sedation, ataxia.
Gabapentin
208
Antiviral: GTP analog that requires activation by thymidine kinase. Used for CMV. Tox: neutropenia. Foscarnet does not require activation.
Ganciclovir, foscarnet
209
Gemfibrozil, clofibrate
Antilipemics: stimulate lipoprotein lipase to convert TGs to FAs. Used in hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia. Tox: liver (increased LFTs), myositis
210
Gentamicin, tobramycin, streptomycin
Aminoglycoside: bactericidal, inhibits formation of initiation complex at the 30S subunit. Used against all aerobic GNRs as in sepsis, and will clear out bowels if given chronically or so intended. Tox: nephrotoxicity (major cause of acute tubular necrosis), ototoxicity, teratogenic.
211
Glipizide, glyburide
Oral hypoglycemics: 2nd generation. Close K + channels on β cells, depolarize cell, cause fusion of insulin vesicles w/ membrane. Tox: hypoglycemia
212
Griseofulvin
Antifungal: interferes w/ microtubules in keratinized tissues. Used in topical dermatophytic infxns.
213
Guanethidine
Postganglionic sympathetic neuron blocker: depletes monoamine stores. Effect reversed by TCAs, cocaine. Tox: severe orthostatic hypotension, sexual dysfunction
214
Haloperidol, fluphenazine, thioridazine, chlorpromazine
Antipsychotic: blocks central dopamine D2 receptors. Used in schizophrenia, psychosis. Tox: EPS effects (acute dystonia, akinesia, akithisia, tardive dyskinesia), hyperprolactinemia, antimuscarinic, anti- α. Less ANS adverse effects than phenothiazines. Neuroleptic malignant syndrome. (“neuroleptics”)
215
Halothane, isoflurane, enflurane, methoxyflurane
General anesthetic: inhaled halogenated hydrocarbon, MOA unknown. Cause myocardial depression, respiratory depression, increased ICP. Halothane is hepatotoxic, enflurane is proconvulsant. All can cause malignant hyperthermia, particularly w/ succinylcholine.
216
Heparin
Anticoagulant: large polymeric molecule with antithrombin, and anti-factor X activity. Rapid onset. Tox: bleeding, HIT, use protamine as antidote. LMW-heparins target Xa w/o PTT monitoring.
217
Antilipemics: stimulate lipoprotein lipase to convert TGs to FAs. Used in hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia. Tox: liver (increased LFTs), myositis
Gemfibrozil, clofibrate
218
Aminoglycoside: bactericidal, inhibits formation of initiation complex at the 30S subunit. Used against all aerobic GNRs as in sepsis, and will clear out bowels if given chronically or so intended. Tox: nephrotoxicity (major cause of acute tubular necrosis), ototoxicity, teratogenic.
Gentamycin, tobramycin, streptomycin
219
Oral hypoglycemics: 2nd generation. Close K + channels on β cells, depolarize cell, cause fusion of insulin vesicles w/ membrane. Tox: hypoglycemia
Glipizide, glyburide
220
Antifungal: interferes w/ microtubules in keratinized tissues. Used in topical dermatophytic infxns.
Griseofulvin
221
Postganglionic sympathetic neuron blocker: depletes monoamine stores. Effect reversed by TCAs, cocaine. Tox: severe orthostatic hypotension, sexual dysfunction
Guanethidine
222
Antipsychotic: blocks central dopamine D2 receptors. Used in schizophrenia, psychosis. Tox: EPS effects (acute dystonia, akinesia, akithisia, tardive dyskinesia), hyperprolactinemia, antimuscarinic, anti- α. Less ANS adverse effects than phenothiazines. Neuroleptic malignant syndrome. (“neuroleptics”)
Haloperidol, fluphenazine, thioridazine, chlorpromazine
223
General anesthetic: inhaled halogenated hydrocarbon, MOA unknown. Cause myocardial depression, respiratory depression, increased ICP. Halothane is hepatotoxic, enflurane is proconvulsant. All can cause malignant hyperthermia, particularly w/ succinylcholine.
Halothane, isoflurane, enflurane, methoxyflurane
224
Anticoagulant: large polymeric molecule with antithrombin, and anti-factor X activity. Rapid onset. Tox: bleeding, HIT, use protamine as antidote. LMW-heparins target Xa w/o PTT monitoring.
Heparin
225
Anticoagulant: large polymeric molecule with antithrombin, and anti-factor X activity. Rapid onset. Tox: bleeding, HIT, use protamine as antidote. LMW-heparins target Xa w/o PTT monitoring.
Heparin
226
Hexamethonium
SNS-plegic: nAChR antagonist. Used in HTN. Tox: orthostatic hypotension, blurred vision
227
Hydralazine
Antihypertensive: increases cGMP to dilate arterioles, reduce afterload. Used in HTN, CHF. Tox: tachycardia, volume retention, SLE-like
228
Hydrochlorathiazide
Thiazide diuretic prototype: blocks Na+/Cl- symporter in distal tubule; Ca2+ is reabsorbed instead. Used in HTN, CHF, chronic calcium stones. Tox: hypokalemia, retention of urate, glucose, lipids, calcium
229
Ibuprofen
NSAID prototype: short duration. Inhibits cyclooxygenase (both I and II) reversibly. Used in arthritis, dysmenorrhea, muscle inflammation. Tox: peptic ulcer, renal damage
230
Imipenem, meropenem
Antibiotic: broad-spectrum carbapenem β- lactam. Penicillinase-resistant. Used for almost all infections except VRE and MRSA. Imipenem is given w/ cilastatin to inhibit renal metabolism. Tox: PCN allergy, seizures in overdose
231
Indinavir, saquinivir, ect
Antiviral: HIV protease inhibitor. Prevents cleavage of polyprotein to produce functional viral enzymes. Tox: buffalo hump or truncal obesity, hyperlipidemia. Ritonavir inhibits P450.
232
Indomethacin
NSAID prototype: highly potent and acute (gout). Closes PDA. Tox: ulcers, renal damage
233
Infliximab
Anti-TF Ab: used in Crohn’s, RA.
234
SNS-plegic: nAChR antagonist. Used in HTN. Tox: orthostatic hypotension, blurred vision
Hexamethonium
235
Antihypertensive: increases cGMP to dilate arterioles, reduce afterload. Used in HTN, CHF. Tox: tachycardia, volume retention, SLE-like
Hydralazine
236
Thiazide diuretic prototype: blocks Na+/Cl- symporter in distal tubule; Ca2+ is reabsorbed instead. Used in HTN, CHF, chronic calcium stones. Tox: hypokalemia, retention of urate, glucose, lipids, calcium
HCTZ
237
NSAID prototype: short duration. Inhibits cyclooxygenase (both I and II) reversibly. Used in arthritis, dysmenorrhea, muscle inflammation. Tox: peptic ulcer, renal damage
Ibuprofen
238
Antibiotic: broad-spectrum carbapenem β- lactam. Penicillinase-resistant. Used for almost all infections except VRE and MRSA. Imipenem is given w/ cilastatin to inhibit renal metabolism. Tox: PCN allergy, seizures in overdose
Imipenem, meropenem
239
Antiviral: HIV protease inhibitor. Prevents cleavage of polyprotein to produce functional viral enzymes. Tox: buffalo hump or truncal obesity, hyperlipidemia. Ritonavir inhibits P450.
Indinavir, saquinivir, ect
240
NSAID prototype: highly potent and acute (gout). Closes PDA. Tox: ulcers, renal damage
Indomethacin
241
Anti-TF Ab: used in Crohn’s, RA.
Inflixamab
242
Ipratropium
Antimuscarinic agent: aerosol for asthma, COPD. Good bronchodilator in 20-30% of patients. 2nd line choice.
243
Isoniazid
Antimycobacterial: inhibits synthesis of mycolic acid. Used as part of treatment regimen or for single prophylaxis of contacts or positive PPD. Fast or slow metabolism by N-acetyltransferase (genetic variability). Tox: peripheral neuropathy (reversed by pyridoxine), G6PD hemolysis, SLE-like, hepatitis
244
Isoproterenol
β1, β2 agonist: bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR. Tox: AV block (rare), angina
245
Ivermectin
Antihelminth: activates worm’s GABA receptor. Used in onchocerciasis (river blindness)
246
Ketamine
Dissociative anesthetic: acts at NMDA glutamate receptor. Stimulates myocardium, excellent analgesic. Tox: hallucination, disorientation, nightmares.
247
Ketoconazole, clotrimazole
Antifungal azole: inhibits fungal P450 to decrease ergosterol synthesis. Used for Candida, dermatophytes and weak systemic mycoses. Used in PCOS to prevent hirsutism (is antiandrogenic). Tox: hepatic dysfunction, inhibits steroid synthesis and P450. Clotrimazole is topical.
248
Labetolol
α- and β-blocker: used in HTN. Tox: AV block, hypotension
249
Lamotrigine
Anticonvulsant: blocks voltage-gated Na+ channels. Used in partial and general seizures. Tox: Stevens-Johnson.
250
Antimuscarinic agent: aerosol for asthma, COPD. Good bronchodilator in 20-30% of patients. 2nd line choice.
Ipratropium
251
Antimycobacterial: inhibits synthesis of mycolic acid. Used as part of treatment regimen or for single prophylaxis of contacts or positive PPD. Fast or slow metabolism by N-acetyltransferase (genetic variability). Tox: peripheral neuropathy (reversed by pyridoxine), G6PD hemolysis, SLE-like, hepatitis
Isoniazid
252
β1, β2 agonist: bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR. Tox: AV block (rare), angina
Isoproterenol
253
Antihelminth: activates worm’s GABA receptor. Used in onchocerciasis (river blindness)
Ivermectin
254
Dissociative anesthetic: acts at NMDA glutamate receptor. Stimulates myocardium, excellent analgesic. Tox: hallucination, disorientation, nightmares.
Ketamine
255
Antifungal azole: inhibits fungal P450 to decrease ergosterol synthesis. Used for Candida, dermatophytes and weak systemic mycoses. Used in PCOS to prevent hirsutism (is antiandrogenic). Tox: hepatic dysfunction, inhibits steroid synthesis and P450. Clotrimazole is topical.
Ketoconazole, clotrimazole
256
α- and β-blocker: used in HTN. Tox: AV block, hypotension
Labetolol
257
Anticonvulsant: blocks voltage-gated Na+ channels. Used in partial and general seizures. Tox: Stevens-Johnson.
Lamotrigine
258
Leuprolide
GnRH analog: agonist when pulsatile, antagonist when continuous. Used for infertility (pulsatile), prostate ca or leiomyoma (continuous). Tox: antiandrogen, N/V.
259
Levodopa/Carbidopa
Dopamine precursor. Used in parkinsonism. Tox: arrhythmia, dyskinesia, resumption of Parkinson symptoms between doses (“on- off” phenomena)
260
Lidocaine, mexetiline, tocainide
Class IB antiarrhythmics. Medium duration amide anesthetic (lido). Shorten AP duration.
Used in ventricular arrhythmias (v-fib, v-tach), as seen post-MI. Tox: CNS
excitation, CV depression
261
Lithium
Antimanic prototype: drug of choice in mania and bipolar affective disorders; blocks phosphatidyl inositol system. Tox: tremor, hypothyroidism, nephrogenic diabetes insipidus, narrow therapeutic index, seizures (in overdose), teratogen (Ebstein’s malformations)
262
Losartan
Angiotensin II receptor blocker. Tox: hyperkalemia, teratogen (fetal kidneys).
263
Lovastatin, "-statin"s
Antilipemic: inhibit HMG-CoA reductase to decrease LDL and increase HDL. Tox: liver damage (elevated LFTs), myositis
264
Mannitol
Diuretic: osmotic action creates large volume of urine. Used in ARF, shock, or to decrease ICP
265
GnRH analog: agonist when pulsatile, antagonist when continuous. Used for infertility (pulsatile), prostate ca or leiomyoma (continuous). Tox: antiandrogen, N/V.
Leuprolide
266
Dopamine precursor. Used in parkinsonism. Tox: arrhythmia, dyskinesia, resumption of Parkinson symptoms between doses (“on- off” phenomena)
Levodopa/Carbidopa
267
Class IB antiarrhythmics. Medium duration amide anesthetic (lido). Shorten AP duration.
Used in ventricular arrhythmias (v-fib, v-tach), as seen post-MI. Tox: CNS
excitation, CV depression
Lidocaine, mexetiline, tocainide
268
Antimanic prototype: drug of choice in mania and bipolar affective disorders; blocks phosphatidyl inositol system. Tox: tremor, hypothyroidism, nephrogenic diabetes insipidus, narrow therapeutic index, seizures (in overdose), teratogen (Ebstein’s malformations)
Lithium
269
Angiotensin II receptor blocker. Tox: hyperkalemia, teratogen (fetal kidneys).
Losartan
270
Antilipemic: inhibit HMG-CoA reductase to decrease LDL and increase HDL. Tox: liver damage (elevated LFTs), myositis
Lovastatin, "-statin"s
271
Diuretic: osmotic action creates large volume of urine. Used in ARF, shock, or to decrease ICP
Mannitol
272
Heterocyclic antidepressant: NE reuptake inhibitor. Tox: sedation, orthostatic hypotension
Maprotiline
273
Meperidine
Opioid analgesic: synthetic and taken orally. Strong agonist at mu opioid receptors, is anti-muscarinic receptors, so it is the drug of choice for cholecystectomy analgesia b/c it prevents sphincter of Oddi spasm.
274
6-mercaptopurine
Antineoplastic: blocks purine synthesis. Used in leukemias & NHL. Myelosuppression increases with allopurinol (metabolized by xanthine oxidase).
275
Metformin
Oral biguanide hypoglycemic: MOA unknown, may inhibit gluconeogenesis. Can be used in DM1. Tox: lactic acidosis
276
Methotrexate
Antineoplastic, immunosuppressant: S-phase specific drug, inhibits dihydrofolate reductase, decreasing dTMP. Tox: Myelosuppression. Leucovorin (folinic acid) rescue used to reduce toxicity after very high doses
277
Metoprolol
β1-selective blocker: used in HTN, CHF, and for prevention of post-MI sudden death, arrhythmias. Tox: bradycardia, AV block, impotence
278
Metronidazole
Antiprotozoal antibiotic: damages bugs by
oxidizing DNA. Used in anaerobic bacterial infections and Giardia, Entamoeba, Trichomonas, Gardnerella. Tox: GI distress, disulfiram-like reaction to alcohol. Subject to P450 inhibition or induction
279
Mifepristone (RU-486)
Progesterone and glucocorticoid inhibitor: abortifacient (implantation requires progesterone). Tox: bleeding, GI disturbances
280
Milrinone, amrinone
Phosphodiesterase inhibitors: increase contractility by increasing cAMP. Used in acute heart failure (as in ICU) only.
281
Opioid analgesic: synthetic and taken orally. Strong agonist at mu opioid receptors, is anti-muscarinic receptors, so it is the drug of choice for cholecystectomy analgesia b/c it prevents sphincter of Oddi spasm.
Meperidine
282
Antineoplastic: blocks purine synthesis. Used in leukemias & NHL. Myelosuppression increases with allopurinol (metabolized by xanthine oxidase).
6-Mercaptopurine
283
Oral biguanide hypoglycemic: MOA unknown, may inhibit gluconeogenesis. Can be used in DM1. Tox: lactic acidosis
Metformin
284
Antineoplastic, immunosuppressant: S-phase specific drug, inhibits dihydrofolate reductase, decreasing dTMP. Tox: Myelosuppression. Leucovorin (folinic acid) rescue used to reduce toxicity after very high doses
Methotrexate
285
β1-selective blocker: used in HTN, CHF, and for prevention of post-MI sudden death, arrhythmias. Tox: bradycardia, AV block, impotence
Metoprolol
286
Antiprotozoal antibiotic: damages bugs by
oxidizing DNA. Used in anaerobic bacterial infections and Giardia, Entamoeba, Trichomonas, Gardnerella. Tox: GI distress, disulfiram-like reaction to alcohol. Subject to P450 inhibition or induction
Metronidazole
287
Progesterone and glucocorticoid inhibitor: abortifacient (implantation requires progesterone). Tox: bleeding, GI disturbances
Mifepristone (RU-486)
288
Phosphodiesterase inhibitors: increase contractility by increasing cAMP. Used in acute heart failure (as in ICU) only.
Milrinone, amrinone
289
Phosphodiesterase inhibitors: increase contractility by increasing cAMP. Used in acute heart failure (as in ICU) only.
Milrinone, amrinone
290
Mirtazapine
Heterocyclic antidepressant: antagonist of α2, central 5-HT receptors. Tox: sedation, weight gain
291
Misoprostol
PGE1 derivative: increases mucus barrier and decreases acid in stomach. Prevents ulcers due to NSAIDs, maintains PDA, induces labor. Tox: diarrhea, abortion.
292
Morphine
Opioid analgesic: strong mu receptor agonist. Poor oral bioavailability. Effects include analgesia, constipation, emesis, sedation, respiratory depression, miosis, and urinary retention. Tolerance may be marked; high potential for psychologic and physical dependence. Additive effects with other CNS depressants. Codeine is a morphine prodrug.
293
Nafcillin, "-oxacillin"s
Penicillinase-resistant penicillin. Used for Staph. Tox: allergy, methicillin is no longer used but caused interstitial nephritis
294
Naloxone
Opioid mu receptor antagonist: used to reverse CNS depressant effects of opioid analgesics (overdose or when used in anesthesia)
295
Neostigmine, physostigmine
Cholinesterase inhibitors. “-stigmines” are carbamates that inhibit cholinesterase by pyridostigmine, edrophonium carbamylation. Neostigmine: used for postop ileus or neuromuscular blockade reversal, treatment of myasthenia gravis. Physostigmine: used for glaucoma (crosses BBB) or atropine overdose. Pyridostigmine: long- acting, used for treatment of myasthenia gravis. Edrophonium: short-acting, used to dx myasthenia gravis.
296
Nevirapine
Nonnucleoside HIV-RT inhibitor: allosteric inhibition. Others: efavirenz, delavirdine. Tox: Stevens-Johnson, induction of P450, insomnia/nightmares
297
Niacin
Antilipemic: reduces VLDL secretion from hepatocytes. Tox: flushing (reduces w/ use)
298
Heterocyclic antidepressant: antagonist of α2, central 5-HT receptors. Tox: sedation, weight gain
Mirtazapine
299
PGE1 derivative: increases mucus barrier and decreases acid in stomach. Prevents ulcers due to NSAIDs, maintains PDA, induces labor. Tox: diarrhea, abortion.
Misoprostol
300
Opioid analgesic: strong mu receptor agonist. Poor oral bioavailability. Effects include analgesia, constipation, emesis, sedation, respiratory depression, miosis, and urinary retention. Tolerance may be marked; high potential for psychologic and physical dependence. Additive effects with other CNS depressants. Codeine is a morphine prodrug.
Morphine
301
Penicillinase-resistant penicillin. Used for Staph. Tox: allergy, methicillin is no longer used but caused interstitial nephritis
Nafcillin, "-oxacillin"s
302
Opioid mu receptor antagonist: used to reverse CNS depressant effects of opioid analgesics (overdose or when used in anesthesia)
Naloxone
303
Cholinesterase inhibitors. “-stigmines” are carbamates that inhibit cholinesterase by pyridostigmine, edrophonium carbamylation. Neostigmine: used for postop ileus or neuromuscular blockade reversal, treatment of myasthenia gravis. Physostigmine: used for glaucoma (crosses BBB) or atropine overdose. Pyridostigmine: long- acting, used for treatment of myasthenia gravis. Edrophonium: short-acting, used to dx myasthenia gravis.
Neostigmine, physostigmine
304
Nonnucleoside HIV-RT inhibitor: allosteric inhibition. Others: efavirenz, delavirdine. Tox: Stevens-Johnson, induction of P450, insomnia/nightmares
Nevirapine
305
Antilipemic: reduces VLDL secretion from hepatocytes. Tox: flushing (reduces w/ use)
Niacin
306
Nifedipine
Calcium channel blocker prototype: vasoselective. Used in angina, HTN. Tox: edema, flushing, (no arrhythmias b/c not cardioactive)
307
Nitroglycerin, nitroprusside
Antianginal vasodilator prototype: releases NO in veins >> arteries. Reduces preload. Used for stable, Prinzmetal angina. Tox: tachycardia, hypotension, headache. Isosorbide nitrate is long- acting version. Nitroprusside has different but similar mechanism, can lead to cyanide toxicity.
308
Nitrosoureas ("-mustine"s)
Antineoplastic: DNA alkylator. Cross BBB, so used in GBM, other brain ca. Tox: CNS.
309
Norepinephrine
Agonist at all α and at β1 adrenoceptors. Used as ICU pressor but sacrifices renal blood perfusion. Causes reflex bradycardia. Tox: renal ischemia, HTN
310
Octreotide
Somatostatin analog. Used in acromegaly, carcinoid, gastrinoma, glucagonoma, VIP- oma, varices
311
Omeprazole
Antiulcer: irreversible blocker of H+/K+ ATPase proton pump in parietal cells of stomach. Used in ZE, GERD, ulcers. Tox: none
312
Ondansetron, granisetron
Antiemetics. “-setrons” are 5-HT3 receptor blockers used for cancer chemotherapy and Metoclopramide for postop N/V. Metoclopramide is a dopamine antagonist at the area postrema.
313
Orlistat
Antiobesity: inhibits pancreatic lipase. Tox: steatorrhea, bloating, fat-soluble vitamin deficiency
314
Calcium channel blocker prototype: vasoselective. Used in angina, HTN. Tox: edema, flushing, (no arrhythmias b/c not cardioactive)
Nifedipine
315
Antianginal vasodilator prototype: releases NO in veins >> arteries. Reduces preload. Used for stable, Prinzmetal angina. Tox: tachycardia, hypotension, headache. Isosorbide nitrate is long- acting version. Nitroprusside has different but similar mechanism, can lead to cyanide toxicity.
Nitroglycerin, nitroprusside
316
Antineoplastic: DNA alkylator. Cross BBB, so used in GBM, other brain ca. Tox: CNS.
Nitrosoureas ("-mustine"s)
317
Agonist at all α and at β1 adrenoceptors. Used as ICU pressor but sacrifices renal blood perfusion. Causes reflex bradycardia. Tox: renal ischemia, HTN
Norepinephrine
318
Somatostatin analog. Used in acromegaly, carcinoid, gastrinoma, glucagonoma, VIP- oma, varices
Octreotide
319
Antiulcer: irreversible blocker of H+/K+ ATPase proton pump in parietal cells of stomach. Used in ZE, GERD, ulcers. Tox: none
Omeprazole
320
Antiemetics. “-setrons” are 5-HT3 receptor blockers used for cancer chemotherapy and Metoclopramide for postop N/V. Metoclopramide is a dopamine antagonist at the area postrema.
Ondansetron, granisetron
321
Antiobesity: inhibits pancreatic lipase. Tox: steatorrhea, bloating, fat-soluble vitamin deficiency
Orlistat
322
Antiobesity: inhibits pancreatic lipase. Tox: steatorrhea, bloating, fat-soluble vitamin deficiency
Orlistat
323
Oxybutin, glycopyrrolate
Antimuscarinic: target GU system to prevent incontinence in quadriplegics
324
Oxytocin
Stimulates labor, uterine contractions, milk letdown.
325
Paclitaxel ("-axel"s)
Antineoplastic: prevents anaphase by “freezing” spindle. Used in female cancers. Tox: myelosuppression.
326
Parathion, malathion, echothiophate
Organophosphate acetylcholinesterase inhibitor: used as insecticide, are poisons. Other
organophosphates: DFP, soman, tabun, Causes “DUMBBLSS”: diarrhea, urination, miosis, bronchospasm, bradycardia, lacrimation, sweating, salivation.
327
Penicillamine
Chelator, immunomodulator: Cu poisoning and sometimes Pb, Hg, As. Used in Wilson’s disease and rheumatoid arthritis
328
Penicillin G
Penicillin. Used against all GP bugs, GNCs. Penicillinase-susceptible. Tox: penicillin allergy, Coombs-positive hemolytic anemia.
329
Phenelzine, trancylcypromine, isocarboxazid
MAOI antidepressant: increase levels of all monoamines. Only used for psychotic
depression due to side effects. Tox: hypertensive crisis with tyramine or meperidine intake, serotonin syndrome with tryptophan ingestion
330
Phenobarbital, thiopental
Barbiturate. Used for sedation, most seizures. Increases duration of GABAA channel opening. Nonteratogenic: 1st line anticonvulsant in pregnancy. Tox: dependence, CNS/respiratory depression (additive), induces P450, induces ALA synthase (cannot be used in porphyrics). Thiopental used for induction of general anesthesia
331
Antimuscarinic: target GU system to prevent incontinence in quadriplegics
Oxybutin, glycopyrrolate
332
Stimulates labor, uterine contractions, milk letdown.
Oxytocin
333
Antineoplastic: prevents anaphase by “freezing” spindle. Used in female cancers. Tox: myelosuppression.
Paclitaxel ("-axel"s)
334
Organophosphate acetylcholinesterase inhibitor: used as insecticide, are poisons. Other
organophosphates: DFP, soman, tabun, Causes “DUMBBLSS”: diarrhea, urination, miosis, bronchospasm, bradycardia, lacrimation, sweating, salivation.
Parathion, malathion, echothiophate
335
Chelator, immunomodulator: Cu poisoning and sometimes Pb, Hg, As. Used in Wilson’s disease and rheumatoid arthritis
Penicillamine
336
Penicillin. Used against all GP bugs, GNCs. Penicillinase-susceptible. Tox: penicillin allergy, Coombs-positive hemolytic anemia.
Penicillin G
337
MAOI antidepressant: increase levels of all monoamines. Only used for psychotic
depression due to side effects. Tox: hypertensive crisis with tyramine or meperidine intake, serotonin syndrome with tryptophan ingestion
Phenelzine, trancylcypromine, isocarboxazid
338
Barbiturate. Used for sedation, most seizures. Increases duration of GABAA channel opening. Nonteratogenic: 1st line anticonvulsant in pregnancy. Tox: dependence, CNS/respiratory depression (additive), induces P450, induces ALA synthase (cannot be used in porphyrics). Thiopental used for induction of general anesthesia
Phenobarbital, thiopental
339
Phenoxybenzamine, phentolamine
α-blocker. Phenoxybenzamine is irreversible, phentolamine is reversible. Used in pheochromocytoma. Tox: orthostatic hypotension
340
Phenylephrine
α1 agonist: pure pressor for ICU shock.
341
Phenytoin (Carbamazepine, Valproate)
Anticonvulsant: blocks neuronal Na+ channels, inhibiting glutamate release from presynaptic excitatory neuron. 1st line for tonic-clonic tx, status epilepticus prophylaxis. Serum levels variable due to first- pass metabolism and dose-dependent nonlinear elimination kinetics. Tox: nystagmus, ataxia, diplopia, sedation, SLE-like, P450 induction drug-binding interactions. Chronic: gingival hyperplasia in kids, peripheral neuropathy, hirsutism, B12 depletion. Teratogen.
342
Pilcarpine
Muscarinic agonist: used as eyedrops for narrow or wide-angle glaucoma. Tox: sweating, salivation
343
Pioglitazone, "-glitazone"s
Oral hypoglycemic: increases insulin sensitivity. Used alone or in combination. Tox: weight gain.
344
Piperacillin, ticarcillin, carbenicillin
GN-active penicillin. Penicillinase- susceptible; given w/ inhibitor. Used for Pseudomonas or other GNRs. Tox: allergy. “Takes Care of Pseudomonas”
345
Pirenzipine, propantheline
Antiulcer: antimuscarinics active on parietal, ECL cells. Tox: tachycardia, dry mouth, diplopia.
346
Piroxicam
NSAID with longest duration of action (t1/2 about 40 h)
347
α-blocker. Phenoxybenzamine is irreversible, phentolamine is reversible. Used in pheochromocytoma. Tox: orthostatic hypotension
Phenoxybenzamine, phentolamine
348
α1 agonist: pure pressor for ICU shock.
Phenylephrine
349
Anticonvulsant: blocks neuronal Na+ channels, inhibiting glutamate release from presynaptic excitatory neuron. 1st line for tonic-clonic tx, status epilepticus prophylaxis. Serum levels variable due to first- pass metabolism and dose-dependent nonlinear elimination kinetics. Tox: nystagmus, ataxia, diplopia, sedation, SLE-like, P450 induction drug-binding interactions. Chronic: gingival hyperplasia in kids, peripheral neuropathy, hirsutism, B12 depletion. Teratogen.
Phenytoin (Carbamazepine, Valproate)
350
Muscarinic agonist: used as eyedrops for narrow or wide-angle glaucoma. Tox: sweating, salivation
Pilocarpine
351
Oral hypoglycemic: increases insulin sensitivity. Used alone or in combination. Tox: weight gain.
Pioglitazone, "-glitazone"s
352
GN-active penicillin. Penicillinase- susceptible; given w/ inhibitor. Used for Pseudomonas or other GNRs. Tox: allergy. “Takes Care of Pseudomonas”
Piperacillin, ticarcillin, carbenicillin
353
Antiulcer: antimuscarinics active on parietal, ECL cells. Tox: tachycardia, dry mouth, diplopia.
Pirenzipine, propantheline
354
NSAID with longest duration of action (t1/2 about 40 h)
Piroxicam
355
NSAID with longest duration of action (t1/2 about 40 h)
Piroxicam
356
Pralidoxime
Acetylcholinesterase regenerator: binds phosphorus in organophosphates toxicity
357
Praziquantel
Antihelminth: causes parasite paralysis by calcium-influx pathway. Used in all fluke and tapeworm infections.
358
Prazosin, terazosin, doxazosin
α1-selective blockers: used in HTN. Tox: first-dose orthostatic hypotension
359
Prednisone
Glucocorticoid prototype: potent, short-acting; much less mineralocorticoid activity than cortisol but more than dexamethasone or triamcinolone. Common in chemotherapy, immunosuppression. May cause apoptosis or inhibit division. Tox: Cushing’s
360
Probenecid
Uricosuric: inhibitor of renal weak acid secretion and reabsorption in S2 segment of proximal tubule; prolongs half-life of penicillin, inhibits reabsorption of uric acid.
361
Probucol
Antilipemic: MOA unknown. Withdrawn but may be effective in preventing restenosis of coronaries after angioplasty. Tox: arrhythmias, decreased HDL
362
Propanolol
Nonselective β-blocker prototype. All β- blockers are also Class II antiarrhythmics, which slow conduction through AV node. Tox: see metoprolol.
363
Propylthiouracil, methimazole
Antithyroid: reduces iodination of tyrosine, MIT/DIT coupling, peripheral T4-to-T3 conversion (T4 is majority but T3 is more active). Tox: rash, agranulocytosis (rare), aplastic anemia.
364
Acetylcholinesterase regenerator: binds phosphorus in organophosphates toxicity
Pralidoxime
365
Antihelminth: causes parasite paralysis by calcium-influx pathway. Used in all fluke and tapeworm infections.
Praziquantel
366
α1-selective blockers: used in HTN. Tox: first-dose orthostatic hypotension
Prazosin, terazosin, doxazosin
367
Glucocorticoid prototype: potent, short-acting; much less mineralocorticoid activity than cortisol but more than dexamethasone or triamcinolone. Common in chemotherapy, immunosuppression. May cause apoptosis or inhibit division. Tox: Cushing’s
Prednisone
368
Uricosuric: inhibitor of renal weak acid secretion and reabsorption in S2 segment of proximal tubule; prolongs half-life of penicillin, inhibits reabsorption of uric acid.
Probenecid
369
Antilipemic: MOA unknown. Withdrawn but may be effective in preventing restenosis of coronaries after angioplasty. Tox: arrhythmias, decreased HDL
Probucol
370
Nonselective β-blocker prototype. All β- blockers are also Class II antiarrhythmics, which slow conduction through AV node. Tox: see metoprolol.
Propanolol
371
Antithyroid: reduces iodination of tyrosine, MIT/DIT coupling, peripheral T4-to-T3 conversion (T4 is majority but T3 is more active). Tox: rash, agranulocytosis (rare), aplastic anemia.
Propylthiouracil, methimazole
372
Prostacyclin
PGI2: vasodilator, inhibitor of platelet aggregation.
373
Quinidine, amiodarone, procainamide, disopyramide
Class IA antiarrhythmics and local anesthetics. Slow Phase 0 and increase firing threshold, increasing AP duration, refractory period. Used for a-fib, a-flutter, v-tach. Tox: cinchonism, torsade (quinidine), SLE-like (procainamide).
Amiodarone is primarily Class III.
374
Quinine, quinidine
Antimalarial: kill blood forms, no effect on liver stages. Tox: cinchonism, positive Coombs test
375
Reserpine
Antihypertensive: depletes monoamine stores. Used in HTN. Tox: sedation, depression
376
Ribavirin
Antiviral: inhibits viral RNA polymerase. Guanosine analog. Used for RSV, influenza, HCV. Tox: hemolytic anemia, teratogen.
377
Rifampin
Antimicrobial: inhibits bacterial RNA polymerase. Used in TB, leprosy, and for contacts of those with meningococcal or H.flu infxn. Tox: orange urine, hepatitis, induces P450.
378
Salmeterol
β2 agonist: inhaled, long-acting for chronic asthma. Tox: arrhythmia, tremor.
379
Scopolamine
Antimuscarinic: centrally-active drug for motion sickness
380
PGI2: vasodilator, inhibitor of platelet aggregation.
Prostacyclin
381
Class IA antiarrhythmics and local anesthetics. Slow Phase 0 and increase firing threshold, increasing AP duration, refractory period. Used for a-fib, a-flutter, v-tach. Tox: cinchonism, torsade (quinidine), SLE-like (procainamide).
Amiodarone is primarily Class III.
Quinidine, amiodarone, procainamide, disopyramide
382
Antimalarial: kill blood forms, no effect on liver stages. Tox: cinchonism, positive Coombs test
Quinine, quinidine
383
Antihypertensive: depletes monoamine stores. Used in HTN. Tox: sedation, depression
Reserpine
384
Antiviral: inhibits viral RNA polymerase. Guanosine analog. Used for RSV, influenza, HCV. Tox: hemolytic anemia, teratogen.
Ribavirin
385
Antimicrobial: inhibits bacterial RNA polymerase. Used in TB, leprosy, and for contacts of those with meningococcal or H.flu infxn. Tox: orange urine, hepatitis, induces P450.
Rifampin
386
β2 agonist: inhaled, long-acting for chronic asthma. Tox: arrhythmia, tremor.
Salmeterol
387
Antimuscarinic: centrally-active drug for motion sickness
Scopolamine
388
Selegiline, entacapone, tolcapone
Dopamine breakdown inhibitors. Selegiline is selective for MAO-B, “-capones” inhibit COMT
389
Sibutramine
Antiobesity: inhibitor of NE, 5-HT uptake. Tox: HTN, tachycardia.
390
Sildenafil
Boner pill: phosphodiesterase inhibitor, causes increased cGMP, relaxation of smooth muscle. Tox: headache, blue/green vision, hypotensive crisis w/ nitrates
391
Somatotropin
GH analog. Used in GH deficiency, Turner’s
392
Sotalol, bretylium, ibutilide
Class III antiarrhythmics. Increase AP duration, refractory period. 2nd line agents for atrial and ventricular arrhythmias. Tox: Sotalol—torsades. Ibutilide—Torsades. Bretylium—arrhythmogenic.
393
Spironolactone, amiloride, triamterene
Diuretics: non-K+-wasting. Spironolactone antagonizes aldosterone activity in collecting tubule. Other 2 block ENaC mobilization by another mechanism. Used in K+-wasting diuresis, hyperaldosteronism, CHF. Spironolactone has antiandrogenic effects (gynecomastia) and can be used in PCOS to prevent hirsutism.
394
Streptokinase
Thrombolytic: accelerates plasminogen-to- plasmin conversion. Tox: bleeding, allergy
395
Succimer (DMSA)
Chelator: dimercaptosuccinic acid; used to chelate Pb and As
396
Dopamine breakdown inhibitors. Selegiline is selective for MAO-B, “-capones” inhibit COMT
Selegiline, entacapone, tolcapone
397
Antiobesity: inhibitor of NE, 5-HT uptake. Tox: HTN, tachycardia.
Sibutramine
398
Boner pill: phosphodiesterase inhibitor, causes increased cGMP, relaxation of smooth muscle. Tox: headache, blue/green vision, hypotensive crisis w/ nitrates
Sildenafil
399
GH analog. Used in GH deficiency, Turner’s
Somatotropin
400
Class III antiarrhythmics. Increase AP duration, refractory period. 2nd line agents for atrial and ventricular arrhythmias. Tox: Sotalol—torsades. Ibutilide—Torsades. Bretylium—arrhythmogenic.
Sotalol, bretylium, ibutilide
401
Diuretics: non-K+-wasting. Spironolactone antagonizes aldosterone activity in collecting tubule. Other 2 block ENaC mobilization by another mechanism. Used in K+-wasting diuresis, hyperaldosteronism, CHF. Spironolactone has antiandrogenic effects (gynecomastia) and can be used in PCOS to prevent hirsutism.
Spironolactone, amiloride, triamterene
402
Thrombolytic: accelerates plasminogen-to- plasmin conversion. Tox: bleeding, allergy
Streptokinase
403
Chelator: dimercaptosuccinic acid; used to chelate Pb and As
Succimer (DMSA)
404
Succinylcholine
Depolarizing paralytic: nAChR antagonist selective for motor receptor. Short duration (5 min). No antidote for Phase 1 (depolarized) block, use neostigmine to reverse Phase 2 (repolarized) block. Contraindicated in any hyperkalemic condition.
405
Sulfasalazine
Immunosuppressant: sulfa drug + ASA derivative, activated in gut. Used in ulcerative colitis, Crohn’s.
406
Sumatriptan
5-HT1D receptor agonists. Vasocontrict, short half-life. Used to abort migraine attacks. other "-triptans" Tox: Prinzmetal- like vasospasm, contraindicated in coronary artery dz
407
Tamoxifen, raloxifen
Estrogen partial agonists ("SERMs"). Used in breast ca, osteoporosis prevention. Tamoxifen increases uterine ca risk.
408
Tetracycline, doxycycline
Antibiotic: blocks amino-acyl tRNA at 30S subunit. Used for zoonoses, Chlamydia UTI, atypical pneumonia. Doxycycline is excreted in feces; can use in CKD patients. Tox: bone deformity and dental discoloration in kids, Fanconi’s syndrome, photosensitivity
409
Thalidomide
Antiinflammatory: decreases TNF production to improve leprosy skin symptoms. Tox: teratogen (causes flipper limbs)
410
Theophylline
Anti-asthma: phosphodiesterase inhibitor favors bronchodilation. Lower therapeutic index. 3rd line agent.
411
Ticlopidine, clopidogrel
Antiplatelet: blocks ADP receptor to prevent aggregation. Prevents strokes, occlusion after angioplasty
412
Depolarizing paralytic: nAChR antagonist selective for motor receptor. Short duration (5 min). No antidote for Phase 1 (depolarized) block, use neostigmine to reverse Phase 2 (repolarized) block. Contraindicated in any hyperkalemic condition.
Succinylcholine
413
Immunosuppressant: sulfa drug + ASA derivative, activated in gut. Used in ulcerative colitis, Crohn’s.
Sulfasalazine
414
5-HT1D receptor agonists. Vasocontrict, short half-life. Used to abort migraine attacks. other "-triptans" Tox: Prinzmetal- like vasospasm, contraindicated in coronary artery dz
Sumatriptan
415
Estrogen partial agonists ("SERMs"). Used in breast ca, osteoporosis prevention. Tamoxifen increases uterine ca risk.
Tamoxifen, raloxifen
416
Antibiotic: blocks amino-acyl tRNA at 30S subunit. Used for zoonoses, Chlamydia UTI, atypical pneumonia. Doxycycline is excreted in feces; can use in CKD patients. Tox: bone deformity and dental discoloration in kids, Fanconi’s syndrome, photosensitivity
Tetracycline, doxycycline
417
Antiinflammatory: decreases TNF production to improve leprosy skin symptoms. Tox: teratogen (causes flipper limbs)
Thalidomide
418
Anti-asthma: phosphodiesterase inhibitor favors bronchodilation. Lower therapeutic index. 3rd line agent.
Theophylline
419
Antiplatelet: blocks ADP receptor to prevent aggregation. Prevents strokes, occlusion after angioplasty
Ticlopidine, clopidogrel
420
Tolbutamide, chlorpropamide
Oral hypoglycemics: older sulfonylurea group. Tox: hypoglycemia, disulfiram-like effect
421
Topiramate
Anticonvulsant: Blocks Na+ channels, increases GABA. Used for general and partial seizures. Tox: sedation, “mental dulling,” kidney stones, weight loss
422
t-PA
Thrombolytic: tissue plasminogen activator. Used in acute MI to recanalize the occluded coronary. Occasionally used in pulmonary embolism, stroke. Tox: bleeding. Antidote is aminocaproic acid
423
Trastuzumab
Antineoplastic: monoclonal Ab against Her2/ neu. Tox: cardiotoxicity.
424
Trazodone
Heterocyclic antidepressant: 5-HT reuptake inhibitor. Tox: sedation, nausea, priapism
425
Trimethoprim-sulfamethoxazole
Antibiotics: cause blockade at dihydrofolate reductase and dihydropteroate synthase. Used for PCP prophylaxis/treatment, Salmonella, pneumonia, chronic UTI. Tox: sulfa reaction including Stevens- Johnson and hemolytic anemia, kernicterus in neonates, may require leucovorin rescue
426
Tropicamide, topical atropine
Antimuscarinic: eyedrops for ophthalmologic mydriasis
427
Tubocurarine
Nondepolarizing paralytic: competitive nAChR antagonist. “-curiums” and “- curoniums” have different structures. Tox: histamine release, hypotension. Reverse blockade w/ cholinesterase inhibitor.
428
Oral hypoglycemics: older sulfonylurea group. Tox: hypoglycemia, disulfiram-like effect
Tolbutamide, chlorpropamide
429
Anticonvulsant: Blocks Na+ channels, increases GABA. Used for general and partial seizures. Tox: sedation, “mental dulling,” kidney stones, weight loss
Topiramate
430
Thrombolytic: tissue plasminogen activator. Used in acute MI to recanalize the occluded coronary. Occasionally used in pulmonary embolism, stroke. Tox: bleeding. Antidote is aminocaproic acid
t-PA
431
Antineoplastic: monoclonal Ab against Her2/ neu. Tox: cardiotoxicity.
Trastuzumab
432
Heterocyclic antidepressant: 5-HT reuptake inhibitor. Tox: sedation, nausea, priapism
Trazodone
433
Antibiotics: cause blockade at dihydrofolate reductase and dihydropteroate synthase. Used for PCP prophylaxis/treatment, Salmonella, pneumonia, chronic UTI. Tox: sulfa reaction including Stevens- Johnson and hemolytic anemia, kernicterus in neonates, may require leucovorin rescue
Trimethoprim-sulfamethoxazole
434
Antimuscarinic: eyedrops for ophthalmologic mydriasis
Tropicamide, topical atropine
435
Nondepolarizing paralytic: competitive nAChR antagonist. “-curiums” and “- curoniums” have different structures. Tox: histamine release, hypotension. Reverse blockade w/ cholinesterase inhibitor.
Tubocurarine
436
Flumazenil
Benzodiazepine antagonist: used to reverse CNS depressant effects of benzos in overdose or in anesthesia
437
Fluoxetine, paroxetine, sertraline, citalopram
SSRI antidepressant. Also used for OCD. Takes effect in 2-3 weeks. Tox: less antimuscarinic, cardiotoxic; more GI distress and sexual dysfunction. Causes serotonin syndrome if used w/ MAOI. Fluoxetine inhibits P450.
438
Benzodiazepine antagonist: used to reverse CNS depressant effects of benzos in overdose or in anesthesia
Flumazenil
439
SSRI antidepressant. Also used for OCD. Takes effect in 2-3 weeks. Tox: less antimuscarinic, cardiotoxic; more GI distress and sexual dysfunction. Causes serotonin syndrome if used w/ MAOI. Fluoxetine inhibits P450.
Fluoxetine, paroxetine, sertraline, citalopram
440
Levodopa/Carbidopa
Dopamine precursor. Used in parkinsonism. Tox: arrhythmia, dyskinesia, resumption of Parkinson symptoms between doses (“on- off” phenomena)
441
Lithium
Antimanic prototype: drug of choice in mania and bipolar affective disorders; blocks phosphatidyl inositol system. Tox: tremor, hypothyroidism, nephrogenic diabetes insipidus, narrow therapeutic index, seizures (in overdose), teratogen (Ebstein’s malformations)
442
Dopamine precursor. Used in parkinsonism. Tox: arrhythmia, dyskinesia, resumption of Parkinson symptoms between doses (“on- off” phenomena)
Levodopa/Carbidopa
443
Antimanic prototype: drug of choice in mania and bipolar affective disorders; blocks phosphatidyl inositol system. Tox: tremor, hypothyroidism, nephrogenic diabetes insipidus, narrow therapeutic index, seizures (in overdose), teratogen (Ebstein’s malformations)
Lithium
444
Phenelzine, trancylcypromine, isocarboxazid
MAOI antidepressant: increase levels of all monoamines. Only used for psychotic
depression due to side effects. Tox: hypertensive crisis with tyramine or meperidine intake, serotonin syndrome with tryptophan ingestion
445
MAOI antidepressant: increase levels of all monoamines. Only used for psychotic
depression due to side effects. Tox: hypertensive crisis with tyramine or meperidine intake, serotonin syndrome with tryptophan ingestion
Phenelzine, trancylcypromine, isocarboxazid
446
Quinine, quinidine
Antimalarial: kill blood forms, no effect on liver stages. Tox: cinchonism, positive Coombs test
447
Antimalarial: kill blood forms, no effect on liver stages. Tox: cinchonism, positive Coombs test
Quinine, quinidine
448
Tolbutamide, chlorpropamide
Oral hypoglycemics: older sulfonylurea group. Tox: hypoglycemia, disulfiram-like effect
449
Tubocurarine
Nondepolarizing paralytic: competitive nAChR antagonist. “-curiums” and “- curoniums” have different structures. Tox: histamine release, hypotension. Reverse blockade w/ cholinesterase inhibitor.
450
Oral hypoglycemics: older sulfonylurea group. Tox: hypoglycemia, disulfiram-like effect
Tolbutamide, chlorpropamide
451
Nondepolarizing paralytic: competitive nAChR antagonist. “-curiums” and “- curoniums” have different structures. Tox: histamine release, hypotension. Reverse blockade w/ cholinesterase inhibitor.
Tubocurarine
452
Valproate (carbamazepine, phenytoin)
Anticonvulsant: 1st line for tonic-clonic. Also used for absence, myoclonic seizures. Blocks Na+ channels, increases GABA. Tox: GI distress, hepatic necrosis (rare), teratogenic (spina bifida)
453
Vancomycin
Antibiotic: bactericidal glycopeptide inhibitor of cell wall synthesis. Binds D-ala residues. Used only against GP bugs, especially MRSA and C. diff. Tox: “red man syndrome” w/ fast infusion, ototoxicity, nephrotoxicity
454
Venlafaxine
Heterocyclic antidepressant: monoamine reuptake inhibitor. Also used for anxiety.
455
Verapamil, diltiazem
Calcium channel (L-type) blocker prototype: has more depressant effect on heart than dihydropyridines (eg, nifedipine). Class IV antiarrhythmics: slow AV nodal conduction for SVT. Tox: AV block, CHF, edema, constipation. “The cardiac-specialized CCBs”
456
Vinblastine, vincristine
Antineoplastic: alkaloid that blocks microtubule polymerization during M phase. Used in lymphoma, Wilms. Tox: myelosuppression. Vincristine – peripheral neuropathy
457
Warfarin
Oral anticoagulant prototype: prevents ɣ- carboxylation of vitamin K-dependent factors (2, 7, 9, 10), making them useless. Tox: bleeding, teratogenic, drug-drug interactions. Antidote: vitamin K, fresh plasma. Monitor PT or INR.
458
Zafirlukast, montelukast
Anti-asthma: block leukotriene receptors. 3rd line agent.
459
Zanamivir, oseltamivir
Antiviral: prevents release of influenza A and B particles from host cells. Used to treat and prophylax both influenzae.
460
Zidovudine (AZT), didanosine (DDI)
Antiviral: nucleoside inhibitor of HIV RT. Inhibit RT and when incorporated cause production of a defective virion. Tox: megaloblastic anemia (AZT), pancreatitis (DDI), peripheral neurpathy (DDI). Can be used during pregnancy to reduce transplacental transmission. Others: lamivudine, stavudine, zalcitabine.
461
Zileuton
Anti-asthma: 5-lipoxygenase inhibitor. 3rd line agent.
462
Anticonvulsant: 1st line for tonic-clonic. Also used for absence, myoclonic seizures. Blocks Na+ channels, increases GABA. Tox: GI distress, hepatic necrosis (rare), teratogenic (spina bifida)
Valproate
463
Antibiotic: bactericidal glycopeptide inhibitor of cell wall synthesis. Binds D-ala residues. Used only against GP bugs, especially MRSA and C. diff. Tox: “red man syndrome” w/ fast infusion, ototoxicity, nephrotoxicity
Vancomycin
464
Heterocyclic antidepressant: monoamine reuptake inhibitor. Also used for anxiety.
Venlafaxine
465
Calcium channel (L-type) blocker prototype: has more depressant effect on heart than dihydropyridines (eg, nifedipine). Class IV antiarrhythmics: slow AV nodal conduction for SVT. Tox: AV block, CHF, edema, constipation. “The cardiac-specialized CCBs”
Verapamil, diltiazem
466
Antineoplastic: alkaloid that blocks microtubule polymerization during M phase. Used in lymphoma, Wilms. Tox: myelosuppression. Vincristine – peripheral neuropathy
Vinblastine, vincristine
467
Oral anticoagulant prototype: prevents ɣ- carboxylation of vitamin K-dependent factors (2, 7, 9, 10), making them useless. Tox: bleeding, teratogenic, drug-drug interactions. Antidote: vitamin K, fresh plasma. Monitor PT or INR.
Warfarin
468
Anti-asthma: block leukotriene receptors. 3rd line agent.
Zafirlukast, montelukast
469
Antiviral: prevents release of influenza A and B particles from host cells. Used to treat and prophylax both influenzae.
Zanamivir, oseltamivir
470
Antiviral: nucleoside inhibitor of HIV RT. Inhibit RT and when incorporated cause production of a defective virion. Tox: megaloblastic anemia (AZT), pancreatitis (DDI), peripheral neurpathy (DDI). Can be used during pregnancy to reduce transplacental transmission. Others: lamivudine, stavudine, zalcitabine.
Zidovudine (AZT), didanosine (DDI)
471
Anti-asthma: 5-lipoxygenase inhibitor. 3rd line agent.
Zileuton
