QB - PHARM Flashcards

1
Q

Pentamidine (3)

A

Pneumocystis jiroveci pneumonia (HIV)
Leishmaniasis
African Sleeping sickness

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2
Q

Nifurtimox

A

Chagas’ disease (Trypanosoma cruzi)

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3
Q

Mebendazole

A

Ascariasis
Trichuriasis
Hookworm
Pinworm

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4
Q

Ivermectin

A

Onchocerciasis (river blindness)

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5
Q

Metronidazole

A

Giardia lamblia
Entamoeba histolytica
Trichomonas vaginalis
C. difficile pseudomembranous colitis

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6
Q

Giardia lamblia

A

Metronidazole

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7
Q

Entamoeba histolytica

A

Metronidazole

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8
Q

Trichomonas vaginalis

A

Metronidazole

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9
Q

C. difficile pseudomembranous colitis

A

Metronidazole

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10
Q

Cloroquine, Mefloquine

A

Plasmodium (malaria)

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11
Q

Primaquine

A

P. vivax

P. ovale

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12
Q

Methotrexate

A

Antifolate (cancer therapy)

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13
Q

Trimethoprim

A

Antifolate (inhibits DHF to THF)

Treats UTI & ear infections

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14
Q

UTI & ear infections

A

Trimethoprim

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15
Q

Imatinib

A

CML (bcr-abl tyrosine kinase inhibitor)

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16
Q

Enoxaparin

A

Low-molecular weight heparin (better bioavailability, longer half-life)

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17
Q

Lepirudin, Bivalirudin

A

derivatives of Hirudin - INHIBITS thrombin (alternative for heparin)

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18
Q

Clopidogrel, Ticlopidine

A

Blocks ADP receptors - prevent binding of gpIIb/IIIa to fibrinogen (NO PLATELET aggregation)

For coronary stenting/acute coronary syndrome

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19
Q

Abciximab

A

Bind DIRECTLY to gpIIb/IIIa on activated platelets - NO PLATELET aggregation

Fibrinogen serves as linker molecule btwn gpIIb/IIIa receptors on two different platelets

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20
Q

Dactinomycin
Doxorubicin
Bleomycin

A

Intercalates DNA - Antitumor antibiotics

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21
Q

Dactinomycin

A

Intercalates DNA - antitumor antibiotics

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22
Q

Doxorubicin

A

Intercalates DNA - Antitumor antibiotics

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23
Q

Bleomycin

A

Intercalates DNA - Antitumor antibiotics

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24
Q

Cyclophosphamide

Nitrosureas

A

Alkylating agents - crosslinks DNA

Cyclophosphamide - solid tumors, leukemia, lymphomas

Nitrosureas - brain tumors

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25
Vincristine, Vinblastine | Paclitaxel
Microtubule inhibitors Vincristine, Vinblastine - block mitotic spindle formation Paclitaxel - mitotic spindle cannot dissolve (stuck in hyperstabilization) - breast/ovarian cancers
26
Cisplatin
Crosslinks DNA Testicular, ovary, bladder cancer; lung carcinomas Nephrotoxic, acoustic nerve damage
27
Etoposide
Inhibit topoisomerase II
28
Hydroxyurea
Inhibit ribonucleotide reductase --> decrease DNA synthesis (S phase) Rx for CML, sickle cell disease
29
Prednisone
CLL, non-Hodgkin's lymphoma
30
Tamoxifen
SERM - selective estrogen receptor antagonist in breast, agonist in bone Raloxifene - no increased risk of endometrial cancer (like Tamoxifen)
31
Trastuzumab (Herceptin)
Breast cancer - cardiotoxic
32
Rituximab
antibody against CD20 Non-hodgkin's lymphoma, rheumatoid arthritis
33
Bevacizumab
Solid tumors monoclonal antibody against VEGF Inhibits angiogenesis
34
Dabigatran, Argatroban
Direct thrombin inhibitors Prolongs TT (without affecting PT or PTT)
35
Heparin
Increases antithrombin binding/neutralization of thrombin & factor Xa (prevents clots) SHORT term management of DVT (deep vein thrombosis)/peri-operative non ambulatory patients
36
Warfarin
Inhibits Vitamin K dependent clotting factors (II, VII, IX, X) Inhibits carboxylation of GLUTAMIC ACID residues Monitor PT/INR LONG TERM prevention of recurrent venous thrombosis
37
Lepirudin, Argatroban
Direct thrombin inhibitors Use for Heparin-induced thrombocytopenia
38
Ticlopidine, Clopidogrel
Inhibit ADP mediated platelet aggregation Unstable angina
39
Rofecoxib
Selective COX2 inhibitor - provides ANTI-INFLAMMATION but does not interfere w/ COX1 (on platelets and in GI tract) Selective COX2 side effect: increased GI bleeding Aspirin = irreversible inhibitor of COX1&2
40
Dapsone, Nitrites effect on blood
Methemoglobinemia (Fe2+ oxidized to Fe3+)
41
Vincristine
Inhibits microtubule formation (M phase) | Neurotoxic --> peripheral neuropathies
42
Topoisomerase I and II inhibitors Hydroxyurea
Inhibits synthesis pathway
43
Ganciclovir
CMV - MOST COMMON use for HIV patients Retinitis, esophagitis, pneumonia polyneuropathy, transverse myelitis, encephalitis
44
Mechanism of Ganciclovir & adverse rxns
Interferes w/ human host cell DNA synthesis (greater effect than acyclovir) Adverse rxns: Neutropenia Anemia Thrombocytopenia
45
What drug used in conjuction w/ Ganciclovir will exacerbate its side effects?
Zidovudine (AZT) AZT used for HIV patients Inhibit some mammalian cellular and mitochondrial DNA polymerases --> bone marrow suppression --> anemia, granulocytopenia AZT + Ganciclovir in HIV patients --> neutropenia & anemia
46
Ampicillin
Listeria monocytogenes | Meningitis in immunosuppressed
47
Amphotericin
Cryptococcus neoformans | Meningitis in AIDS patients
48
Risperidone
Schizophrenia Side effect: hyperprolactinemia --> amenorrhea
49
Colchicine
Inhibits tubulin polymerization into microtubules -- impairs neutrophil mitosis --> decrease neutrophil motility Disrupts membrane-dependent functions (chemotaxis and phagocytosis) Treats GOUTY arthritis Side effect = abdominal pain, nausea, diarrhea
50
Avoid using colchicine in what kind of patients?
Elderly w/ renal dysfunction
51
Terbinafine
Inhibits squalene epoxidase --> NO ergosterol SYNTHESIS Rx for dermatophytosis
52
Amphotericin B | Nystatin
BINDS to ergosterol - makes holes in CELL MEMBRANE
53
Caspofungin
``` Echinocandin class (INHIBITS CELL WALL synthesis) Blocks synthesis of B(1,3)-D-glucan ```
54
Rx for Candida & Aspergillus
Caspofungin
55
Flucytosine
Antimetabolite 5-FU in fungal cell - inhibits protein synthesis via RNA miscoding Cryptococcal infections (given w/ amphotericin B) Fungal infections
56
Rx of Endometriosis
Leuprolide | Danazol
57
Metyrapone
Inhibits production of cortisol | See ACTH surge then product buildup of 11-deoxycortisol (17-OH corticosteroids in urine)
58
Rx for gouty arthritis
1. Indomethacin (NSAID) 2. Colchicine (acute relief - inhibits neutrophil migration into inflamed areas) 3. Allopurinol (prevention of gout - lowers serum uric acid)
59
Indomethacin; mechanism? Uses?
Close patent ductus arteriosus (lowers prostaglandins) COX1 & COX2 inhibitor -- suppresses prostaglandin synthesis --> anti-inflammatory agent & pain reliever
60
Rx for septic arthritis
Ceftriaxone - gonococcus infection
61
Somatosatin analogs
Octreotide | Lanreotide
62
Acarbose; what enzyme is inhibited?
Inhibits a-glucosidase Impairs hydrolysis of sugars (limits postprandial absorption of sugars)
63
Metformin
Increase sensitivity of target tissue to insulin
64
Rosiglitazone (a thiazolidinedione)
Similar to metformin (biguanide)
65
Enalapril
ACE inhibitor - decreases diabetic proteinuria
66
Glyburide
Sulfonylurea that increases rate of insulin secretion (can see C peptide levels increase as insulin secretion increases)
67
Colchicine
Acute management of GOUT Interfere w/ adhesion molecules & microtubule formation responsible for neutrophil chemotaxis and phagocytosis --> reduce inflammation! Side effect: diarrhea, nausea/vomiting (hence only use colchicine when patients have contraindication to NSAIDs -- peptic ulcer/renal failure patients)
68
Glucocorticosteroids (for gout)
Acute gout - inhibits Phospholipase A2 activity --> less inflammation
69
What two drugs are contraindicated in acute gouty attacks?
Probenecid Allopurinol May exacerbate symptoms
70
Probenecid
Probenecid - Decrease proximal tubular uric acid reabsorption (decrease uric acid levels) Rx for gout
71
Allopurinol
Allopurinol - Inhibition of xanthine oxidase Rx for gout
72
Pioglitazone
A type of thiazolidnediones (TZDs) Binds peroxisome proliferator activated receptor (PPAR-gamma) --> increase ADIPONECTIN synthesis (low levels of adiponectin seen in type II diabetes) Adiponectin decreases insulin resistance Side effects: fluid retention, weight gain, precipitation of congestive heart failure
73
Action of adiponectin
Decreases insulin resistance Rx for diabetics
74
Exenatide
Glucagon like polypeptide (GLP-1) Decrease additional release of glucagon Increase insulin release Induce satiety Decrease gastric emptying (slow rate of sugar absorbed from foods to enter into blood circulation) DECREASE blood glucose
75
Major side effects of following drugs: 1. Etanercept 2. Methotrexate or Leflunomide 3. Amiodarone 4. Hydroxychloroquine 5. NSAIDs
1. Etanercept: TNF-a inhibitor to treat RA/psoriasis/psoriatic arthritis -- need PPD skin test (more susceptible to infectious agents) 2. Methotrexate or Leflunomide -- Hepatotoxic 3. Amiodarone - Pulmonary fibrosis 4. Hydroxychloroquine - Ophthalmologic 5. NSAIDs - GI blood loss
76
TNF-alpha inhibitors for RA treatment
Infliximab Etanercept Adalimumab
77
Infliximab
TNF-alpha inhibitors -- RA treatment
78
Etanercept
TNF-alpha inhibitors -- RA treatment
79
Adalimunab
TNF-alpha inhibitors -- RA treatment
80
Inhibitors of purine/pyrimidine synthesis for RA treatment
Methotrexate Leflunomide Azathioprine
81
Methotrexate
Inhibitors of purine/pyrimidine synthesis -- RA treatment
82
Leflunomide
Inhibitors of purine/pyrimidine synthesis -- RA treatment
83
Azathioprine
Inhibitors of purine/pyrimidine synthesis -- RA treatment
84
Chlorthalidone
Thiazide diurectic Increase Ca2+ resorption in early distal collecting tubule of nephron
85
Clomiphene
Selective estrogen receptor modulator PREVENTS negative feedback inhibition on hypothalamus --> increased FSH and LH release (infertility treatment for women who want to ovulate and get pregnant)
86
Mitotane
Adrenocorticolytic drug -- for adrenocortical carcinoma
87
Spironolactone
Androgen receptor antagonist - inhibits testosterone synthesis Treats acne & hirsutism Gynecomastia & testicular atrophy in men Also a K+ sparing diuretic
88
Other drugs (other than spironolactone) to treat hirsutism
Flutamide (testosterone receptor antagonist) Finasteride (5-alpha-reductase inhibitor)
89
Haloperidol, Fluphenazine
blocks D2 receptors (dopamine) --> strong cholinergic influence (M1 receptor mediated) EXTRAPYRAMIDAL effects: acute dystonic reactions (muscle spasms, tongue protrusions/twisting, eyes deviated upwards) akathisia (inner restlessness, can't sit still) parkinsonism
90
Diphenhydramine, Benztropine
M1 receptor antagonist re-establish dopaminergic-cholinergic balance used to treat extrapyramidal effects
91
Flumazenil
GABA antagonist - counter acute overdoses of Benzodiazepine
92
Chlorpromazine, Clozapine
H1-histamine receptor | Sedation
93
Chlorpromazine, Thioridazine
Low potency antipsychotics Anticholinergic side effects = confusion, dry mouth, urinary retention Blocks central and peripheral muscarinic cholinergic receptors
94
Flutamide
Competes w/ testosterone and DHT for receptors on prostate tumors (prevents androgen-receptor binding on tumors --> tumors shrink in size) Need to be administered w/ GnRH agonist Side effect (androgen depletion): hot flashes, gynecomastia, impotence
95
GnRH agonists
Leuprolide, goserelin, nafarelin, histrelin binds GnRH receptors in anterior pituitary -- inhibit LH and FSH decreased LH --> decreased Leydig cell stimulation --> diminished testosterone
96
Ketoconazole
Decrease synthesis of steroid hormones in gonads/adrenals
97
Anastrozole
Decreased peripheral androgen aromatization - blocks estrogen production selectively Treatment of postmenopausal women w/ breast cancer (their greatest source of estrogen is conversion of androstenedione in the adrenal glands to estrone in liver, muscle, fat VIA aromatization
98
Finasteride
Inhibits 5-a-reductase Decrease conversion of testosterone to DHEA (dihydrotestosterone) - also abbreviated DHT discordant decrease in DHT
99
Alpha-glucosidase inhibitors
Acarbose and Miglitol Decrease disaccharidase activity at intestinal brush border --> less carbohydrate absorption Side effect: flatulence, bloating, abdominal pain, rash
100
Sulfonylurea (mechanism)
Membrane ion channels
101
Insulin (mechanism)
Surface TYROSINE KINASE-coupled receptors
102
Glucagon-like polypeptide (GLP-1)
Secreted by intestinal L cells (response to food intake) Induces satiety, decrease gastric emptying, increase insulin release GLP-1 acts through cell surface receptors coupled to G protein-adenyl cyclase system E.g. Exenatide (long acting GLP-1) for DIABETES type II
103
Bisphosphonates
Osteoporosis, Paget's disease of bone, malignancy-induced hypercalcemia Structural analogs of pyrophosphate - compoent of hydroxyapatite "-DRONATE" endings Alendronate, Risedronate, Ibandronate Bisphosphonates make hydroxyapatite more INSOLUBLE - also decrease bone resorption by interfering w/ osteoclasts Patients need to stay upright for at least 30 mins. to prevent reflux; given in fasting state w/ plenty of water Be mindful of use in RENAL failure patients
104
OA
Morning stiffness for <30mins (shorter than RA patients) Bony swelling of DIP and PIP Use-dependent joint pain in weight bearing joints (alleviated w/ rest)
105
Tamoxifen | Raloxifene
SERMs: have different effect on estrogen levels in different tissues Breast - antiestrogenic effect Bone - partial estrogen agonist (minimizes bone resorption effect - treats osteoporosis in post menopausal women) **Endometrium - estrogen agonist (increase incidence of endometrial cancers) Serum: normalizes LDL (somewhat improves lipid profile) Other concerns: Thromboembolic disease
106
Amiodarone
Class III anti-arrhythmic Side effects: a) Prolong QT interval (K+ mediated repolarization) b) THYROID dysfunction -- induces HYPOthyroidism (treat w/ LEVOTHYROXINE) c) blue-gray skin discoloration d) corneal micro-deposits e) drug-related hepatitis
107
Long term treatment for gouty arthritis (tophaceous gout)
Uricosuric drugs (avoid in renal failure pts): Probenecid Sulfinpyrazone Xanthine oxidase inhibitors: Allopurinol** (best)
108
Zileuton
Lipoxygenase inhibitor Allergic rhinitis & bronchial asthma
109
Treatment for Gonorrhea vs. Chlamydia
``` Gonorrhea = Ceftriaxone Chlamydia = Azithromycin or Doxycycline ```
110
Thiazolidinediones (TZDs)
Decrease insulin resistance by acting on PPAR-gamma --> increase adiponectin levels in type II diabetes PPAR-gamma activation --> increase fat mass secondary to increased differentiation of preadipocytes into mature adipocytes (adiponectin is cytokine secreted by adipocytes) Side effect: fluid retention, weight gain, CHF due to fluid retention
111
Rituximab
CD20+ non-Hodgkin's lymphoma - B cells
112
Infliximab
binds TNF-alpha (involved in inflammatory response) TNF is intercellular signaling protein RA, Crohn's disease
113
Certolizumab
TNF-alpha | also for autoimmune diseases
114
Imatinib
Philadelphia chromosome positive chronic myelogenous leukemia kit-positive GIST (gastrointestinal stromal tumors)
115
Vancomycin resistance
D-Ala-D-Ala to D-Ala-D-Lac
116
Valproate risk
Neural tube defects (inhibit intestinal folic acid absorption)
117
Dantrolene
Malignant hyperthermia
118
Breast cancer
Doxorubicin (cardiotoxic)
119
Acetazolamide
Carbonic anhydrase inhibitor - PROXIMAL TUBULE --> block reabsorption of HCO3- --> increased urinary pH --> metabolic acidosis (since there's no bicarb around to buffer) BAD for kid with diabetes who is admited in acidosis state
120
Indications for Acetazolamide
Diuretic (proximal tubule) Open-angle and close-angle glaucoma (decrease HCO3- and aqueous humor formation) --> relieve pressure
121
Side effects of Acetazolamide
Somnolence Paresthesias Urine alkalinization*
122
Macrolides
Cholestatic hepatitis
123
Quinolones
Tendon rupture
124
Tetracyclines in kids
Staining of teeth
125
Benzodiazepines
Short: 24hrs TRIAZOLAM - short acting (avoid daytime sleepiness) - treats anxiety/insomnia/acute seziures/alcohol withdrawal LORAZEPAM - intermediate DIAZEPAM, FLURAZEPAM - long acting (excessive daytime fatigue, impaired judgement)
126
Phencyclidine (PCP)
NMDAR inhibition (NMDA is receptor for excitatory neurotransmitter glutamate) Moderate use - feelings of detachment + distance Paranoia, hallucinations Very hostile and aggressive
127
Heroin
Opiate | Euphoria, constricted pupils, lethargy, clammy skin, nausea
128
Amphetamine
NE effects Used for ADHD Rapid heart rate, high BP, anxiousness, sweating, tremors, dry mouth, hallucinations
129
Coacine
Inhibits reuptake of dopamine, NE, serotonin Blurry vision, tremors, twitching, chest pain, irritability, hallucinations/delusions, high BP+HR
130
Diazepam
CNS depressant Confusion, mild amnesia, sedation, slurred speech, low BP and HR
131
Lysergic acid diethylamide (LSD)
Serotonin receptor agonist Hallucinations --> delusions --> severe paranoia
132
Marijuana
Contains tetrahydrocannabinol (THC) Euphoria, short term memory loss, perception distortion Silliness, red eyes, slowed reflexes, dizziness, impaired coordination
133
Beta blockers
Used for relieving tachycardia + chest pain in atherosclerotic coronary artery disease patients (reduce BP and cardiac work, HR) Noncardioselect agents precipitate asthma symptoms = bad! B1 - SLOWS heart rate B2 - bronchoconstriction + wheezing
134
Reserpine
Inhibits dopamine entry into presynaptic vesicles = chemical sympathectomy
135
Guanethidine
Inhibit NE release --> LOWER BP and HR
136
Tricyclic antidepressants | Cocaine
Inhibit NE reuptake --> INCREASE NE concentration at presynaptic neurons --> constant stimulation Sympathomimetic: Precipitate ANGINA (coronary artery vasoconstriction) + MI Cocaine causes INCREASED BP, chest pain, agitation, mydriasis, DRAMATIC symmetric pupillary dilation that remains responsive to light, tachycardia Nasal mucosal atrophy, partial septum destruction = patient uses cocaine
137
Phenelzine
MAO inhibitor (decreases rate of inactivation of neurotransmitters by monoamine oxidase --> INCREASE concentration of serotonin, NE, dopamine) dietary restriction: cheese, wine
138
Sertaline
SSRI (selective serotonine reuptake inhibitor) Co-administration w/ MAO inhibitor could result in SEROTONIN SYNDROME: restlessness, hyperreflexia, diaphoresis, tremors (excessive serotonin) Need to wait 2 weeks after MAO inhibitor discontinuation before beginning SSRI - gives body chance to replenish monoamine oxidase stores (monoamine oxidase responsible for breaking down monoamine neurotransmitters)
139
Desmopressin uses
Vasopressin (ADH) - used for diabetes insipidus High dose: increases factor VIII activity in hemophilia A treats vWF disease
140
Leuprolide
analog of GnRH continuous administration - suppresses LH and FSH initial transient phase of increase in both testosterone & DHT --> stable decrease in testosterone & DHT prostatic cancer, precocious puberty, endometriosis
141
Finasteride
Antiandrogen | BPH via inhibition of a-reductase
142
Ondansetron
Antiemetic | blocks 5-HT3 seroton receptors
143
Flutamide
Prostate cancer | androgen inhibitor
144
Octreotide
Somatostatin analog | Controls symptoms of carcinoid syndrome (flushing, wheezing, diarrhea, syncope)
145
Sodium valproate
Absence & tonic-clonic seizures Ethosuximide also good for absence seizures (does NOT treat tonic-clonic)
146
Carbamazepine
Blocks Na channels (less propagation of action potential) Complex partial seizures Generalized tonic-clonic seizures Trigeminal neuralgia BIPOLAR side effect: - AGRANULOCYTOSIS or aplastic anemia (bone marrow suppression) - Hepatotoxic - SIADH
147
Phenytoin
Blocks Na+ channels prolonging rate of recovery (increase refractory period -- blocks further action potentials from firing) Tonic-clonic seizures STATUS EPILEPTICUS Side effects: lymphadenopathy, hirsutism, coarsening of facial features, acne, gingival hypertrophy
148
Lithium toxicity
Nephrogenic diabetes insipidus Monitor TSH and BUN
149
Foscarnet
Treats CMV in HIV patients (Can also use ganciclovir, cidofovir) Ganciclovir first line treatment for CMV RETINITIS (but side effect = neutropenia) so shouldn't give to HIV pt. in bone marrow suppression state already (due to Zidovudine) Side effect: HYPOcalcemia, HYPOphosphatemia, HYPOmagnesium Foscarnet wastes Mg2+ --> DECREASE PTH release --> decrease calcium LOW Ca2+ and Mg2+ --> seizures*
150
Acyclovir
Treatment for HSV-2 Nucleoside analog - incorporates into viral DNA chain --> terminates DNA synthesis Nephro + Neurotoxic Delirium/tremor
151
Lamivudine toxicity
Nucleoside reverse transcriptase inhibitor (NRTI) for HIV peripheral neuropathy lactic acidosis
152
Indinavir usage & toxicity
Protease inhibitor (HIV) fat redistribution hyperglycemia (insulin resistance) hypertriglyceridemia
153
Furosemide, Torsemide, Bumetanide
``` Loop diuretics (ascending loop of Henle) Na-K-2Cl symporter blocked ``` Otoxicity
154
HCTZ, chlorthalidone
``` Thiazide diuretic (blocks Na-Cl in DCT) for edema secondary to HF, renal disease, liver disease ``` Hyperuricemia Hypercalcemia*
155
Triamterene, Spironolactone, Amiloride
K+ sparing diuretic (collecting tubule) Hyperkalemia
156
Acetazolamide
Carbonic anhydrase inhibitor (PCT) Metabolic acidosis (blocks reabsorption of NaHCO3)
157
Mannitol
Osmotic diuretic - descending limb of Henle's loop & proximal tubule Hypernatremia Pulmonary edema
158
ACE inhibitors
decreases efferent arteriole of kidneys from constriction decreases GFR used for HTN, HF, renal failure patients
159
Atorvastatin
HMG-CoA reductase inhibitor muscle toxicity hepatic dysfunction
160
Metformin (acid-base effect)
Lactic acidosis
161
Prazosin
selective alpha-1 adrenergic antagonist Uses: HTN Urinary retention (due to BPH) side effect: HYPOtension (postural hypotension)
162
Rituximab
anti-CD20 B-cell lymphomas rheumatoid arthritis
163
Infliximab
IgG antibody to TNF-alpha Rheumatoid arthritis Ankylosing spondylitis Crohn's disease
164
IL-2
Renal cell carcinoma | Melanoma
165
Imatinib
CML Philadelphia chromosome BCR/ABL protein tyrosine kinase
166
Omalizumab
anti-IgE | asthma
167
Abciximab
gp IIb/IIIa receptor antagonist blocks final step of platelet aggregation administered during angioplasty in patients w/ acute coronary syndrome
168
Cetuximab
``` anti-EGFR non-small cell lung cancer CRC pancreatic cancer squamous cell carcinoma (head and neck) ```
169
Bevacizumab
anti-VEGF metastatic colon/renal carcinoma non-small cell lung cancer recurrent glioblastoma multiforme
170
Muromonab-CD3 (OKT3)
anti-CD3 antibodies treatment of acute rejection in patients w/ kidney, heart, liver transplants anti-CD3 antibodies bind to and inhibit T lymphocytes
171
Amifostine
free radical scavenger decrease nephrotoxicity when using Cisplatin (platinum containing chemo drug that crosslinks DNA causing acute renal tubular injury) decrease nephrotoxicity w/ alkylating chemo agents
172
Leucovorin
Folinic acid methotrexate (MTX) overdose
173
Filgrastim
G-CSF analog stimulate proliferation and differentiation of granulocytes; used to minimize granulocytopenia after myelosuppressive chemo
174
Dexrazoxane
Iron chelator prevent anthracycline-induced (doxorubicin) cardiotoxicity (CHF)
175
Fomepizole
ANTIDOTE for ethanol (rubbing alcohol) or ethylene glycol (antifreeze) poisoning
176
Raltegravir
HIV integrase inhibitor (HIV can't integrate into host genome and use host machinery to make more viral mRNA)
177
Maraviroc
CCR5/CXCR4 antagonist
178
Ritonavir, Saquinavir
Protease inhibitor (HIV)
179
Enfuvirtide
Fusion inhibitor (HIV) prevents viral attachment to cells
180
Lamivudine, Tenofovir, Efavirenz
RT inhibitor (HIV)
181
Desmopressin
Release of factor VIII and vWF from endothelial cells Treats Hemophilia A (bleeding into joints - hemarthrosis) also ADH analog - treats diabetes insipidus (increase reabsorption of H20 in collecting tubules)
182
Metoclopramide
Dopamine antagonist (D1 receptor causes vasodilation/relaxation of smooth muscles/vessels) Gastro-prokinetic (increase gastric emptying in patients w/ gastroparesis) Treats nausea and vomiting Migraine headache
183
NNRTI
Nevirapine, Efavirenz, Delavirdine NNRTI: inhibits RT of HIV - prevent incorporation of DNA copy of viral genome into host DNA
184
Ropinirole
Non-ergoline dopamine agonist Restless legs syndrome D2, D3, D4 dopamine agonist w/ highest affinity for D3 metabolized by P450 CYP1A2
185
Alprazolam
Short acting BENZO Moderate to severe anxiety and panic attacks Anxiety associated w/ depression
186
Zolpidem
Short acting BENZO | For insomnia, sleeping on overseas plane trip
187
Hemicholinium
Inhibits uptake of choline - prevents formation of Ach
188
Vesamicol
Inhibits packaging of Ach into transport vesicles
189
Botulinum toxin
Blocks release of Ach (flaccid paralysis)
190
Metyrosine
Blocks conversion of tyrosine to DOPA
191
Reserpine
Blocks packaging of Dopamine/NE into vesicles
192
Guanethidine, Bretylium
Blocks release of NE
193
Cocaine TCAs Amphetamine
Blocks reuptake of NE
194
Amphetamine
Stimulates NE release | Blocks reuptake of NE
195
H1 blockers (1st generation)
Diphenhydramine Chlorpheniramine Dimenhydrinate Allergy Motion sickness Sleep aid Sedation, antimuscarinic, anti-alpha-adrenergic
196
H1 blockers (2nd generation)
Loratadine Fexofenadine Allergy Decrease CNS entry (less sedative effect)
197
Albuterol
Relaxes bronchial smooth muscle (B2)
198
Salmeterol, Formoterol
Long acting B2 agonist (prophylaxis) Tremor, arrhythmia (side effects) Be careful using w/ heart disease patients that may be on B-blocker
199
Theophylline
Inhibits phosphodiesterase -- decrease cAMP hydrolysis -- bronchodilation NARROW TI = cardiotoxic & neurotoxic Metabolized by P450 Blocks adenosine
200
Beclomethasone | Fluticasone
Corticosteroids - Inhibit synthesis of cytokines Inactivate NF-kB (TNF-a not made, no other inflammatory agents) 1st line therapy for chronic asthma
201
Montelukast | Zafirlukast
block leukotriene D4 receptors for chronic asthma prophylaxis
202
Zileuton
5-lipoxygenase pathway inhibitor block conversion of arachidonic aicd to leukotrienes
203
Omalizumab
monoclonal anti-IgE antibody - inhibits IgE binding to mast cells used in allergic asthma
204
Guaifenesin
Thins respiratory secretions (does not suppress reflex)
205
N-acetylcysteine
mucolytic - can loosen mucus plugs in CF patients antidote for acetaminophen toxicity prevents radiocontrast-induced nephropathy in patients w/ renal insufficiency
206
Bosentan
Treats pulmonary arterial HTN antagonize endothelin-1 receptors --> decrease pulmonary vascular resistance
207
Dextromethorphan
Antitussive (antagonize NMDA glutamate receptors) Codeine analog Naloxone given for overdose
208
Pseudoephedrine | Phenylephrine
Sympthomimemtic alpha-agonistic nasal decongestant Pseudoephedrine also as a stimulant Open obstructed eustachian tubes Toxicity - HTN, CNS stimulation/anxiety
209
Methacholine
Muscarinic receptor agonist | Asthma challenge testing
210
Amphotericin B | Nystatin
polyene antifungal | BINDS ergosterol --> pore formation and cell lysis
211
Terbinafine
inhibits squalene-2,3-epoxidase (ultimately decrease ergosterol synthesis) accumulates in skin & nails treats dermatophytoses
212
Griseofulvin
enters fungal cells | binds microtubules --> inhibits microtubules
213
Caspofungin | Micafungin
block 1,3-beta-D-glucan synthesis (polysaccharide component of fungal CELL WALL)
214
Flucytosine
inhibits DNA replication and RNA (protein synthesis) in fungal cells synergistic w/ amphotericin B ** cryptococcal meningitis
215
Ketoconazole, Fluconazole
INHIBIT SYNTHESIS of ergosterol ``` P450 inhibitor (increase conc of other drugs in system) Increase toxicity: warfarin cyclosporine tacrolimus phenytoin isoniazid rifampin oral hypoglycemics ```
216
Cyclosporine
Decrease IL-2 synthesis --> inhibit T cell proliferation | immunosuppressant (transplant pts)
217
Chloramphenicol
Inhibits bacterial peptidyltransferase (cant transfer aa from A to P site - can't form peptide bonds)
218
Streptomycin
Inhibit INITIATION complex formation | Binds and distorts prokaryotic 30S ribosomal subunit
219
Clindamycin | Erythromycin
Inhibit TRANSLOCATION
220
Tetracycline
Inhibit aminoacyl-tRNA binding in A site
221
Isoniazid + rifampin +streptomycin, ethambutol, and/or pyrazinamide
M. tuberculosis treatment
222
Cromolyn | Nedocromil
Inhibit mast cell DEGRANULATION prevention/prophylactic treatment aspirin hypersensitivity/exercise-induced asthma, seasonal allergies
223
Glucocorticoids (asthma)
Inhibit phospholipase A2 --> inhibit formation of arachidonic acid --> NO prostaglandins (from COX) & leukotrienes (from lipoxygenase)
224
Isoproterenol
B1 and B2 adrenergic agonist Increase HR, CO Decrease peripheral arterial resistance Bronchodilation in asthmatics Indicated in asthma, COPD (but not in pt. with MI)
225
Selective B-blocker (A-M) vs Non-selective B-blocker (N-Z)
Selective (A-M) B-blockers don't have pulmonary effects: better for pts. with pre-existing PULMONARY issues Non-selective: B2 blocker causes BRONCHOCONSTRICTION, peripheral VASOSPASM, predispose diabetics to HYPOglycemia
226
TB treatment
Rifampin (inhibits bacterial DNA-dependent RNA polymerase) - inhibits transcription + isoniazid + pyrazinamide + ethambutol and/or streptomycin
227
Lithium toxicity
Hypothyroidism - measure TSH levels regularly Nephrogenic diabetes insipidus Teratogenic (Ebstein's anomaly)
228
Valproic acid toxicity
Hepatitis | Teratogenicity
229
Fluphenazine
Extrapyramidal symptoms (tardive dyskinesia later on)
230
Clozapine
Treats delusions/hallucinations Atypical antipsychotic: acts on D4 receptors (instead of D2 recepors) -- not likely to cause dopaminergic side effects (pseudoparkinsonism, tardive dyskinesia, hyperprolactinemia) Side effects: Agranulocytosis Seizures
231
Risperidone
Atypical antipsychotic Side effect: Hyperprolactinemia
232
Carbamazepine: side effect
Agranulocytosis
233
Which antipsychotic causes prolonged QT?
Ziprasidone
234
Treatment for absence seizures
Ethosuximide | Sodium valproate
235
Anticonvulsant therapy
Diazepam, Lorazepam, Midazolam
236
Treatment for gneralized tonic-clonic seizures
Phenobarbital
237
Treatment for complex partial seizures or generalized tonic-clonic seizures
Carbamazepine
238
Methylphenidate
Indirect-acting sympathomimetic ADHD disorder Narcolepsy
239
Rapid acting insulins
Lispro Aspart Glulisine Action starts in 15 minutes Peaks at 45-75 minutes
240
Regular (short) acting insulins
Action starts in 30 mins Peaks at 2-4 hours Lasts 5-8 hours Given SQ Used to treat DKA (hypotension, tachycardia in young patient w/ diabetes type I)
241
Intermediate acting insulin
NPH Starts working in 2 hours Peaks 4-12 hours Lasts 18 hours
242
Long acting insulin
Detemir Contains fatty acid side chain that binds to albumin = prolonged action Works within 2 hrs Peaks 3-9 hrs Lasts up to 24 hrs
243
Slow release insulin
``` Glargine insulin analog (long duration of action) ``` Lasts 24hrs
244
Allopurinol | Rasburicase
Reduce uric acid levels during tumor lysis syndrome Prevent acute renal failure in pts. undergoing chemo for high grade lymphomas/leukemias
245
Denosumab
prevents osteoclast activation (prevents bone loss) | prevents RANKL and RANK interaction
246
Folinic acid (Leucovorin)
Reverse toxicities of MTX (methotrexate) on GI and bone marrow
247
Amitriptyline
TCA block muscarinic receptors receptors (anti-cholinergic) overdose mimics ATROPINE toxicity
248
Adverse effect of nonselective B-adrenergic blockers
Masked symptoms of hypoglycemia Bradyarrhythmias Worsening of Raynaud phenomenon CNS depression
249
Treatment to prevent recurrence of HSV-2
Oral daily valacyclovir, acyclovir, famciclovir after incidence
250
Ethosuximide
Blocks T-type Ca2+ channels in thalamic neurons --> hyperpolarization Absence seizures
251
Drug that mimics atropine toxicity
Amitriptyline (+ other TCAs) Antimuscarinic fever, cutaenous flushing, dry oral mucosa, dilated poorly reactive pupils, confusion
252
Prazosin toxicity
a1-adrenergic blocker treats HTN and urinary retention (due to BPH) side effect: postural hypotension
253
Side effect of nonselective B-adrenergic blockers
masked symptoms of hypoglycemia in diabetics worsening of Raynaud phenomenon
254
selective alpha-1 blockers (preference for using these)
no alpha2 blockage (alpha-2 suppresses sympathetics) selective alpha1 blockage causes less tachycardia
255
Lamivudine
NRTI Treatment of HIV-1 and HIV-2
256
Valacyclovir Acyclovir Famciclovir
HSV-2 positive Tzanck smear genital vesicular rash
257
MTX and 5-FU both inhibit thymidylate formation; what drug can be used to overcome MTX
Leucovorin (N5-formyl-THF) bypasses DHF reductase -- overcome MTX Leucovorin potentiates 5-FU by strengthening thymidylate synthase MTX: inhibits DHF reductase 5-FU: stabilizes THF & thymidylate syntheatse --> less thymidylate synthetase available for thymidine synthesis
258
Drug-induced Parkinsonism can be side effect of antipsychotics; treatment of drug induced Parkinsonism?
Anticholinergics (benztropine and trihexylphenidyl) for patients w/ drug-induced Parkinsonism Levodopa contraindicated - precipitate psychosis Dopamine agonists (bromocriptine) - used in idiopathic Parkinsonism BUT NOT in drug-induced Parkinsonism (can exacerbate underlying psychosis)
259
Mechanism of -statin drugs | e.g. Atorvastatin
Statins inhibit HMG CoA reductase --> DECREASE cholesterol synthesis by liver Body responds by increasin gLDL receptors on hepatocytes to increase LDL uptake from circulation (therefore decreasing LDL circulating in blood)
260
Side effects of Haloperidol; why can't you give it to patients w/ drug-induced Parkinsonism?
Haloperidol = first gen. antipsychotic = dopamine-receptor blocker (causes Parkinsonian symptoms) Extrapyramidal side effects
261
What drug is used to noramlize prolactin levels and prevent amenorrhea-galactorrhea?
Dopamine agonists (Bromocriptine)
262
Drugs that decrease VLDV
Fibrates and nicotinic acid therapy Decrease hepatic production of VLDL --> treatment for primary hypertriglyceridemia (increased VLDL)
263
Ezetimibe
Decrease intestinal absorption of dietary cholesterol
264
Biliary excretion of cholesterol increase or decrease in patients on statins?
Biliary excretion of cholesterol DECREASES in pts. on statins due to decreased synthesis of cholesterol in liver
265
Treatment for generalized anxiety disorder; why does this drug have low abuse potential?
Buspirone - selective agonist of 5HT(1A) receptor Dependence does not occur Reduced potential for abused compared to Benzodiazepines
266
Amphotericin B
Systemic candidiasis
267
Nystatin
Oral candidiasis "swish and swallow" binds to ergosterol in fungal cell membrane --> formation of pores and leakage of ungal cell contents
268
Griseofulvin
inhibits fungal cell mitosis @ metaphase | indicated for treatment of dermatophytoses
269
Penicillins
B lactam antibiotics | Inhibit peptidoglycan cross-links in bacterial cell wall
270
Terbinafine
``` Accumulates in skin, nails, adipose tissue treat dermatophytosis (onychomycoses) ```
271
Nicotinic acid (Niacin) use; side effects?
Niacin (vitamin B3) treatment of dyslipidemia - Decrease synthesis of VLDL and hepatic triglycerides - Decrease conversion of VLDL to LDL - Increase HDL Cutaneous symptoms -- flushing, warmth, itching mediated by prostaglandins (pre-treatment w/ ASA helps symptoms)
272
Skin side effect of Vancomycin
Red man syndrome - histamine release
273
Serotonin precursor
Tryptophan
274
Serotonin importance in neuro drugs
Serotonin = mood regulation Selective serotonin reuptake inhibitors --> increase serotonin levels --> people happier (antidepressant medication)
275
Statins: MOA
inhibiting enzyme HMG-CoA reductase | upregulation of hepatocyte LDL receptors --> increased uptake of LDL cholesterol from circulation
276
Bile acid-binding resins mechanism
Cholestyramine Colestipol binds bile acid -- intereferes w/ hepatic recycling/reabsorption of bile acids hepatic cholesterol used in order to re-synthesis more bile acids (since there's no bile acids around) -- increased uptake of LDL from circulation to make bile acids
277
Bile acid-binding resins (side effects)
Constipating & bloating Malabsorption of vitamin K Hypertriglyceridemia -- do not use w/ patients that already have hypertrigylceridemia!! Exacerbate diverticulosis (due to constipating side effect) Gallbladder stones
278
Niacin (vitamin B3) - relation to GI
Inhibit hepatic VLDL production | Used to increase HDL levels
279
Drug of choice for alcohol withdrawal
Long-acting benzodiazepines (chlordiazepoxide, diazepam) Short-acting benzodiazepines (lorazepam, oxazepam) preferrer for advanced liver dysfunction
280
Mechanism by which drugs given in alcohol withdrawl works?
Give GABA agonists such as barbituates or benzodiazepines (similar effect as alcohol) alcohol withdrawl symptoms: patient who has been in hospital and hasn't had access to alcohol --> CNS excitation (since there's no alcohol to stimulate GABA receptors) --> tremulousness, insomnia, anxiety, headache, autonomic hyperactivity (variable BP, diaphoresis, tachycardia)
281
Baclofen
GABA agonist -- spastic conditions
282
Haloperidol (toxicity)
lowers serizure threshold
283
Phenobarbital
barbituate anticonvulsant - enhances GABA activity
284
Treatment for active tuberculosis
``` Rifampin Ethambutol Isoniazid Pyrazinamide and/or Streptomycin ```
285
Rx for atypical mycobacterial infections (e.g. Mycobacterium avium complex)
Macrolide + Rifampin + Ethambutol
286
Rx for Staph endocarditis
IV nafcillin + aminoglycoside (gentamicin)
287
Bacterial resistance to rifampin -- mechanism?
genetic mutation of bacterial DNA-dependent RNA polymerase Rifampin needs to be administered as part of multi-drug regimen P450 inducer (other drugs will be metabolized more rapidly w/ co-administration with rifampin)
288
Mycobacterial resistance to isoniazid?
Catalase-peroxidase or Genetic modification of isoniazid binding site on mycolic acid synthesis enzyme
289
Resistance to ethambutol
Inhibit synthesis of mycobacterial cell wall via increase production of arabinosyl transferase
290
Resistance to Pyrazinamide
Lowers the environmental pH to kill M. tuberculosis | Drug has to be converted to active form via pyrazinamidase (bacterial mutate this enzyme)
291
Mechanism of digoxin on AV conduction
Decrease AV nodal conduction via increased paraympathetic tone (vagus nerve --> decrease rate of AV conduction --> ventricles contract at more normal rate --> adequate fiastolic filling time --> normal cardiac output) *prevents rapid ventricular response (usually accompanying a. fib) -- which leads to poor CO and backup of blood in lungs (heart failure)
292
Digoxin effect on ventricular contractility
blockade of NA-K-ATPase on cardiac myocytes --> increased itracellular Ca2+ levels in sarcoplasmic reticulum --> maximal crosslinking of actin and myosin --> increased ventricular contractility
293
Isoniazid can lead to deficiency of which enzyme?
Vitamin B6 (pyridoxine) Isoniazid chemically similar to B6: competes w/ B6 to make GABA --> defective product Peripheral neuropathy Drug also increases excretion of B6 Need to give supplemental B6 with Isoniazid
294
Chronic treatment to prevent bronchial asthma
Fluticasone (inhaled glucocorticoid) Cortiscosteroids = strongest effect on inflammatory compoenent of astham (steroids usually end in "-sone")
295
Action of glucocorticoids on lungs
Not for treat of acute episodes of asthma inhibit formation of cytokines responsible for asthma apoptosis of inflammatory cells (macrophages, lymphocytes, eosinophils) decrease amount of mucus produced by goblet cells reduce airway hyperresponsiveness by decreasing inflammation
296
Nifedipine
DHP Ca2+ channel blocker Treats HTN Blocks Ca2+ influx into bronchial smooth muscle cells --> bronchodilation
297
Acyclovir use
Herpes simplex infections
298
Clarithromycin + other antibiotics
Mycobacterium avium complex
299
Leukocyte interferon-a
hepatitis B and C hairy cell leukemia condyloma acuminatum (HPV) Kaposi's sarcoma
300
Pentamidine
Pneumocystis pneumonia
301
Sulfonylurea or meglitnide abuse - action on blood sugar
Increase insulin, c-peptide, pro-insulin levels bind to ATP-dependent K+ channels on pancreatic beta cells --> inhibit hyperpolarizing potassium current --> depolarization --> Ca2+ channels opening --> exocytosis of secretory granules filled w/ mature insulin & c-peptide
302
Main site of action of nitroglycerin
Venodilator --> large veins Treats angina by venodilating --> blood collects in venous system --> decrease preload --> decrease ventricular wall stress --> decrease cardiac O2 demand
303
Vessels in which nifedipine and prazosin works
Nifedipine (Ca2+ channel blocker) Prazosin (alpha1-adrenergic blocker) Small arteries and arterioles -- primary site of hormonal regulation of systemic blood pressure and primary vascular site of action of vasoactive antihypertensive drugs
304
Absence of lamellar bodies of type II pneumocytes
Patchy alveolar atelectasis (collapse) | Neonatal respiratory distress syndrome
305
Methotrexate (MTX) - mechanism & additional drugs given in conjunction w/
Inhibits DHF reductase --> block folinic acid synthesis Can be given w/ Leflunomide & TNF-a inhibitors for rheumatoid arthritis
306
Side effects of MTX
Stomatitis (painful mouth ulcers) - supplement w/ folic acid Hepatotoxicity Myelosuppression (increased risk for opportunistic infections) B cell lymphomas Pulmonary fibrosis contraindicated in pregnancy
307
Side effects of Naproxen
GI bleeding fluid retention worsening HTN
308
Minocycline
Treats early mild rheumatoid arthritis photosensitivity (mild side effect)
309
Hydroxychloroquine
main use - SLE can be used for early mild seronegative rheumatoid arthritis permanent retinal damage (serious adverse)
310
Corticosteroid chronic use - side effects?
weight gain hyperglycemia bone density, skin striae, proximal muscle weakness used w/ NSAIDs -- potentiate risk for GI bleeding
311
Valproic acid
blocks NMDA receptors - affects K+ current can also affect Na+ channels and GABA receptors
312
Similar mechanism of: Phenytoin Carbamazepine Valproic acid
reducing Na+ channels' abiltiy to recover from inactivation
313
Phenoxybenzamine (indication); also effect on insulin
long acting alpha-blocker used for pheochromocytoma blockage of alpha-receptors --> unopposed beta effects --> increase beta2-adrenergic stimulation = increase insulin release
314
Diphenhydramine
Antihistamine (blocks H1 histamine receptor) | Anticholinergic activity
315
Propranolol
Non-cardioselective beta blocker inhibits insulin secretion -- increase risk of diabetes mellitus for patients on long term beta blocker use
316
Drug used to decrease severity of inflammation and decrease extraocular volume in Grave's opthalmopathy
Prednisone (high dose glucocorticoid)
317
Rx that inhibits thyroid peroxidase; how?
Methimazole Propylthiouracil Responsible for oxidation (organification) of iodide to iodine at apical-colloid interface Iodine + tyrosine (on thyroglobulin) --> T1, T2, T3 thyroxin
318
TCA overdose - cause of death?
TCAs inhibit reuptake of NE and serotonin Inhibit fast Na+ channels --> arrhythmias (phase 0 prolonged, prolonged WRS complex) --> negative inotropy --> decrease contractility, refractory hypotension, peripheral vasodilation --> v. fib
319
Rx that causes serotonin syndrome; symptoms?
MAO inhibitor + SSRI (or large doses of SSRI) hyperthermia, autonomic instability, muscle rigidity, myoclonus, diaphoresis
320
Examples of TCAs
Imipramine Amitryptyline Clomipramine
321
Treatment for TCA overdose
Normal saline | Hypertonic sodium bicarbonate
322
Mechanism of Warfarin
inhibits vitamin K dependent g-carboxylation of glutamic acid residues of clotting factors II, VII, IX, X
323
Reversal of warfarin-induced anticoagulation
``` Fresh frozen plasma (rapid reversal) vitamin K (re-synthesis of clotting factors) ```
324
Reversal of heparin
Protamine (binds to heparin and inactivates it)
325
Aminocaproic acid
Antifibrinolytic - inhibits fibrinolysis (inhibits plasminogen)
326
Acylclovir mechanism of action
Guanosine analog Needs to be activated by viral thymidine kinase (TK) acyclovir monophosphate --> phosphorylated to active form --> impairs viral DNA polymerase-mediated replication of virus Rx for HSV-1&HSV2 Related drugs: Famciclovir Valaciclovir EBV and CMV do not have same thymidine kinase as HSV - so drug is not as effective
327
Medroxyprogesterone (Depo Provera)
Progesterone-only contraceptive via IM injection once every 12 weeks
328
Medroxyprogesterone acetate
Decreases endometrial hyperplasia (decrease risk of endometrial carcinoma) Good for postmenopausal women on estrogen replacement Long-acting contraceptive Side effect: decreased bone mineral density
329
Raloxifene
Estrogen agonist: bone, cardiovascular, blood lipoproteins Estrogen antagonist: breast, uterus
330
Alendronate
Synthetic bisphosphonate (analog of pyrophosphate) bone resorption inhibitor
331
Leuprolide
GnRH analog agonist - pulsatile administration antagonist - continuous administration agonist - estrogen levels increase (protect against osteoporosis) antagonist - estrogen levels decrease (protect against breast cancer in post-menopausal women)
332
Cholestyramine Colestipol Colesevelam
Bile acid-binding resins - binds bile acid in GI tract - interferes w/ enterohepatic circulation LDL reduced (hepatic cholesterol used up to make new bile acids) --> increased uptake of LDL from circulation (lowering LDL from blood) side effect: hypertriglyceridemia, VLDL increase usually given w/ a statin (but at least 4 hrs apart so that bile-acid resin doesn't interfere w/ absorption of statin)
333
Gemfibrozil | Fenofibrate
decrease serum triglycerides by reducing hepatic triglyceride production Fibrates activate PPAR-alpha --> PPAR-alpha activates lipoprotein lipase decreased VLDL cholesterol (decreases LDL) decreased TRIGLYCERIDES increase HDL
334
Halothane | Sevoflurane
Have bronchodilation properties -- preferred in patients w/ asthma (since inhalation anesthetics tend to cause postoperative atelectasis via suppression of muciliary clearance)
335
Fluorinated anesthetics - effect on cerebral blood flow
Increase cerebral blood flow (via decreased vascular resistance) --> increased intracranial pressure -- bad!
336
Side effects of inhlation anesthetics
Increased cerebral blood flow --> increased ICP myocardial depression, hypotension respiratory depression decreased renal function
337
Symptoms of opioid withdrawal in an infant born to mom who abuses opioids
Pupillary dilatation Rhinorrhea, sneezing, nasal stuffiness Diarrhea Chills, tremors, jittery movements
338
Treatment of choice for acute opioid withdrawal in neonate
Tincture of opium or paregoric
339
Naloxone
Opioid receptor antagonist Rx for acute opioid intoxication or overdose DO NOT give to patients w/ opioid withdrawal -- can cause seizures
340
Folic acid (folate)
RBC production Lowers homocysteine levels Prevents neural tube defects
341
Sodium bicarbonate
IV - treatment for acidosis and hyperkalemia | Oral - alkalinizing agent/antacid
342
Treatment regimen for M. tuberculosis
Isoniazid - mycolic acid synthesis - disturbs cell wall - disturbs ability of mycobacteria to have acid fast reaction on stain Ethambutol - inhibit mycobacterial cell wall synthesis (no effect on creation of mycolic acid) Rifampin - halts protein synthesis via inhibition of bacterial DNA dependent RNA polymerase -- prevents transcription of DNA into mRNA
343
Where does acetazolamide work?
Proximal convulated tubule | Carbonic anhydrase inhibitor
344
Site of action of loop diuretics; what are they?
Thick ascending limb of loop of Henle Furosemide Bumetanide Torsemide Ethacrynic acid
345
Site of action of thiazide diuretics; side effect?
Distal convoluted tubule Exacerbates hypokalemia
346
What renal drugs has potential to cause hypokalemia?
Loop diuretics (except K+ sparing ones)
347
What type of neuro/psych drug causes diabetes insipidus?
Lithium -- treats bipolar disease Lithium inhibits action of vasopression (ADH) --> polyuria & polydipsia
348
Vancomycin resistance: D-ala-D-ala substitution for mutated sequence; what is the sequence?
D-ala-D-lactate
349
What renal drug should be given to patient w/ HTN and CHF who also has osteoporosis?
Hydrochlorothiazide -- increases absorption of Ca2+ (distal convoluted tubule) Reabsorption also prevents painful renal stones (from hypercalciuria)
350
Where does Ca2+ reabsorption take place in renal tubules? What drug causes this?
Distal convoluted tubule -- Hydrochlorothiazide
351
Site of action between osmotic diuretics & loop diuretics?
Osmotic diuretic - descending limb of loop of Henle & proximal tubule (mannitol) Loop diuretic - thick ascending limb of loop of Henle (furosemide)
352
Furosemide
Loop diuretic -- treats HTN and CHF Increases urinary Ca2+ LOSS --> worsens osteoporosis in post-menopausal women
353
Spironolactone
Inhibits testosterone (and other steroid hormones) Used for antiandrogenic action --> treats hirsutism & androgen-dependent malignancies
354
Acarbose
Oral hypoglycemic agents Rx for type 2 diabetes mellitus
355
Substance in sunscreen to block UVB light
Para-aminobenzoic acid (PABA) esters | Protects against UVB (290-320nm wavelength)
356
What drug is used to diagnose asthma in pt. who presents w/ asthma symptoms but has normal spirometry values?
Methacholine challenge Methacholine = muscarinic cholinergic agonist --> bronchoconstriction + increased airway secretions Administration of Methacholine --> decrease FEV1 by more than 20% indicates bronchial asthama
357
Varenicline
Partial agonist at nicotinic acetylcholine receptors; only releases limited downstream - LESS stimulation of reward pathways (than nicotine) Helps patients w/ cessation of tobacco (reduces withdrawal cravings; attenuating rewarding effects of nicotine)
358
Antidepressant that does NOT cause sexual dysfunction; what are side effects?
Bupropion - does not have sexual dysfunction side effect has stimulatory effect --> treatment for depression w/ associated psychomotor retardation/hypersomnia treats nicotine dependence side effect: agitation, insomnia, seizures
359
Trazodone
highly sedating anti-depressant (helpful for pts. w/ insomnia) causes priapism
360
Antimetabolite = folate antagonist
Methotrexate
361
Antimetbolite - purine analogs
6-MP Fludarabine (for CLL) Cladribine (for hairy cell leukemia)
362
Cladribine
for Hairy Cell Leukemia | Resistant to adenosine deaminase (adenosine functions in purine disposal pathway)
363
Antimetabolite - pyrimidine analogs
5-FU Capecitabine Cytarabine Gemcitabine
364
Lomustine
Nitrosurea DNA alkylation & cross-bridge formation Requires non-enzymatic hydroxylation Penetrates CNS
365
Dacarbazine
Cell-cycle nonspecific methylating agent
366
Cisplatin
Pt-containing chemotherapeutic agent -- forms cytotoxic metabolite in environments w/ low chloride concentration
367
Mercaptopurine
Converted to active metabolite by HGPRT Inactivated by xanthine oxidase
368
What is administered before bronchoscopy to decrease respiratory mucous secretions & promote bronchodilation?
Atropine
369
Mechanism of atropine
Anti-muscarinic (anti-parasympathetics) ``` symptoms of toxicity: flushed skin, hyperthermia (atropine fever) mydriasis & cycloplegia bronchodilation tachycardia constipation, urinary retention ```
370
Mechanism of physostigmine
Anti-acetylcholinesterase --> increases Ach concentrations Tertiary amine - capable of crossing blood-brain barrier (contrast w/ neostigmine & edrophonium -- quaternary ammonium structure LIMITS CNS penetration) Used to reverse atropine toxicity
371
Significance of HMG-CoA reductase; what drugs target this enzyme?
Statins -- inhibit HMG-CoA reductase -- reduce LDL cholesterol HMG-CoA reductase converts HMG-CoA to cholesterol
372
What drugs taken w/ a statin will increase susceptibility to myopathy (muscle pain + increased serum creatine kinase)?
Statins + fibrates (gemfibrozil or fenofibrate) Statins alone increase risk of myopathy & hepatitis Simvastatin - highest associated risk of myopathy Gemfibrozil - increase concentration of statins Fenofibrate - causes myopathy by itself
373
Cholestyramine + statin use common; why must they be dosed at least 4hrs apart?
Cholestyramine (bile acid sequestrant) reduces GI absorption of statins
374
Combination of fibric acid derivatives + bile acid-binding resins increases risk for?
Cholesterol gallstones (increased cholesterol concentration in bile)
375
First line treatment for hypertriglyceridemia
Fibrates
376
Mechanism of niacin
Improves hyperlipidemia by decreasing synthesis of hepatic triglycerides & VLDL Used in conjunction w/ fibrates to lower TGs
377
First line treatment for hypercholesterolemia
Statins - inhibits HMG-CoA reductase Use Ezetimibe to inhibit absorption of cholesterol (if pts. need additional help lowering cholesterol)
378
Why is ACE-I or ARB preferred for diabetics?
Slow progression of diabetic nephropathy (decrease progression to ESRD) Antihypertensive effect
379
Doxazosin Prazosin Terazosin
alpha-1 blocker treats HTN and BPH
380
Pt. w/ pre-existing coronary arter disease + CHF + HTN; what type of cardioselective beta blockers is needed?
Metoprolol | Atenolol
381
Hydrochlorothiazide (HCTZ) indications
1st line med for essential HTN pts. w/ osteoporosis (increases Ca2+) Isolated systolic HTN
382
What drug combinations can increase likelihood of gallstone formation?
Gemfibrozil & cholestyramine Cholestyramine: binds bile acid --> dumps it into bile (increases cholesterol content of bile --> gallstone formation); the good thing about binding bile acids is that liver has to use up LDL to make new bile acids, thus LOWERING LDL in circulation (at the expense of increase risk of gallstone formation) Gemfibrozil - increase cholesterol content of bile (decrease liver synthesis of TGs)
383
MOA for Ondansetron, Granisetron, Dolasetron
Blocks vagus-mediated naseau/vomiting (vagal terminals w/ 5-HT3 receptors initiate vagus n. activity in medulla oblongata's "vomit center") Blocks serotonin in chemoreceptor trigger zone Good for preventing chemo-induced vomiting
384
Mifepristone (RU-486)
Anti-progestin Anti-glucocorticoid Used as abortifacient
385
Danazol
synthetic androgen treats endometriosis treats hereditary angioedema ``` side effects: hirsutism masculinization fluid retention weight gain ```
386
Drug mechanism of statins vs. bile acid-binding resins
Statins: inhibit HMG CoA reductase --> no cholesterol synthesis --> liver increases LDL receptors on surface to uptake LDL (cholesterol source) from circulation --> this lowers cholesterol in blood Bile acid-binding resins: Inhibits reabsorption of bile acids --> liver has to make new bile acids by consuming liver cholesterol; also takes up LDL from circulation as cholesterol source to make more bile; statins taken together w/ bile acid-binding resins to avoid this effect
387
Why is it good to give patient that w/ severe pain and severe hematuria Celecoxib?
Celecoxib is an NSAID and selective COX-2 inhibitor Does NOT have side effects of bleeding & GI ulceration (platelets only express COX-1)
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Both traditional NSAIDs as well as selective COX-2 inhibitors can exacerbate what condition?
Fluid retention --> HTN
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Where is COX-2 expressed (other than platelets)?
Vascular endothelial cells & vascular smooth muscle cells --> vascular DILATATION
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What protacyclin is increased by COX-2?
PGI2 --> anticoagulation and vascular dilatation
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Mechanism of ASA
Irreversibly inhibiting platelet aggregation via ACETYLATION of serine residues of platelet COX enzymes
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What Rx (mucarinic Ach antagonists) is used to treat obstructive diseases such as asthma and COPD?
Tiotropium Ipratorpium Drugs decrease mucus secretion, decrease bronchoconstriction by inhibit muscarinic Ach receptors (parasympathetics)
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Serious side effects of statins?
Myopathy (increase serum CK --> muscle pain = rhabdomyolysis) Hepatitis
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Metabolism of statins through what system?
With exception of PRAVASTATIN, all statin drugs metabolized by P-450 system
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Nausea, vomiting associated w/ levodopa use; mechanism? How do you avoid these symptoms?
Peripheral conversion of levodopa --> DOPAMINE Take Carbidopa (dopa-decarboxylase inhibitor) to limit peripheral conversion of levodopa --> decrease nausea and vomiting
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Rx for plasmodium species
Chloroquine = Plasmodium in bloodstream Primaquine = latent P. vivax and P. ovale in liver
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Dietary restrictions & drug-drug interactions of monoamine oxidase inhibitors (MAOIs); examples of MAOIs?
Restrictions = cheese, wine Drug-drug interactions w/ SSRI Phenelzine Tranylcypromine
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Indication of Phenelzine
Atypical depression/resistant depression Mood reactivity Leaden fatigues (arms and legs feel heavy) Increased sleep and appetite
399
Rx for auditory hallucinations
Schizoprenia Rx: Haloperidol, Chlorpromazine
400
Bimodal distribution in drug metabolism of Isoniazid; why?
Isoinazid metabolized by ACETYLATION See bimodal distribution (2 peaks) of drug metabolism: correlates w/ SLOW and FAST acetylators; slow acetylators at higher risk of adverse reactions
401
What drug used for inflammatory disorders of bowel and skin is metabolized via METHYLATION?
6-mercaptopurine
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Common Rx used for invasive MRSA infections?
Vancomycin Daptomycin Linezolid
403
Vancomycin: MOA and adverse effects?
Blocks glycopeptide polymerization via binding to D-ala-D-ala Adverse: Red man syndrome Nephrotoxicity
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Daptomycin: MOA and adverse effects?
Depolarization of cellular membrane Adverse: Myopathy --> CPK elevation Inactivated by pulmonary surfactant
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Linezolid: MOA and adverse effects?
Inhibits bacterial protein synthesis by binding 50S subunit Adverse: Thrombocytopenia Optic neuritis High risk for serotonin syndrome
406
What is the effect on K+ levels in blood when patient is using drugs that decrease aldosterone secretion (e.g. ACE inhibitors)?
Less aldosterone secretion --> less Na+ retention Na+ and K+ always go in opposite ways Less Na+ retention --> more K+ retention --> hyperkalemia ACE inhibitors (eg. Lisinopril) decrease amount of aldosterone secreted -- predispose to HYPERKALEMIA; more intense hyperkalemia when ACE inhibitor used w/ K+ sparing diuretics (amiloride, triamterene, spironolactone) Pts. with renal insufficiency (more hyperkalemia) or pts. taking K+ supplements
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Specific beta-1 blockers | A-M -- "olol"
Decrease contractility & HR | Inhibit renin release --> antihypertension
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Indapamide
Thiazide diuretic | Blocks Na+-Cl symporters in distal tubules
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Amlodipine: MOA
DHP Ca2+ channel blocker Blocks vascular smooth muscle --> peripheral vasodilation, improved coronary blood flow DHP causes SIGNIFICANT vasodilatoin --> REFLEX TACHYCARDIA; can also cause peripheral edema
410
Morphine: effect on blood vessels
Vasodilator Increases venous capacitance Decrease systemic vascular resistance CNS sympatholytic Can treat ischemic chest pain; esp. during acute MI
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Medications that can cause HYPERKALEMIA
Non-selective B-blockers (N-Z olol) - inhibits beta-2 mediated intracellular K+ uptake ACE inhibitors ARBs K+ sparing diuretics - block epithelial Na+ channel (ENaC) or aldosterone receptor Cardiac glycosides (digoxin) - inhibits Na+/K+ ATPase pump NSAIDs - impaired local prostaglandin synthesis --> reduced renin & aldosterone secretion
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Didanosine; use & adverse rxn?
HIV RT inhibitor Adverse rxn: pancreatitis
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Injection of a substance causes blanching of vein, induration & pallor of tissues surrounding IV site -- what is occuring? What substance is injected? How can this be prevented?
NE infusion --> NE extravasation --> a1 receptor mediated vasoconstriction --> local tissue necrosis Tissue necrosis can be prevented by local injection of alpha-1 blocking drug (e.g. phentolamine)
414
Enalapril
ACE inhibitor CHF HTN Diabetic nephropathy
415
Isoniazid side effects
Hepatocyte damage Peripheral neuropathy (need to simultaneously administer pyridoxine)
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Indication & major toxicity: Statins
High LDL toxicity: hepatitis, myopathy
417
Indication & major toxicity: Niacin
Low HDL ``` toxicity: cutaneous vasodilation HYPERglycemia (acanthosis nigricans) HYPERuricemia/gout hepatitis ```
418
Indication & major toxicity: Fibric acid derivatives | Gemfibrozil & fenofibrate
High TG toxicity: gallstones myopathy (worse when combined w/ statins)
419
Indication & major toxicity: Bile acid-binding resins (Ezetimibe)
High LDL toxicity: GI upset Hypertriglyceridemia Malabsorption
420
Rx for benign prostatic hyperplasia and HTN
alpha-1 blockers | Doxazosin, Prazosin, Terazosin
421
Common side effect of K+ sparing diuretics
Gynecomastia (more common w/ spironolactone use than eplerenone)
422
DHP vs. non-DHP Ca2+ channel blocker
DHP Ca2+ channel blocker: selective for vascular smooth muscle -- vessels! (eg. Amlodipine) Non-DHP Ca2+ channel blocker: selective for heart (Verapamil)
423
Indications for ribavirin
Nucleoside analog - inhibits guanine nucleotides RSV or Hep C
424
Oseltamivir
sialic acid analogue inhibitor influenza A & B neuraminidases
425
Amantadine
Impairs UNCOATING of influenza A virion after it is endocytosed by host cell
426
What drug may precipitate opioid withdrawal when used w/ morphine?
Pentazocine (weak opiod narcotic - produces analgesic effects w/ little abuse potential) Partial agonist activity and weak antagonist activity at mu receptors; when used w/ other selective mu receptor agonists (eg morphine) --> pentazocine can compete w/ other mu AGONISTS and produce ANTAGONISTIC effect -- Opioid narcotics = selective mu receptor AGONISTS
427
Rx for sickle cell anemia; mechanism of drug?
Hydroxyurea increases HbF synthesis Gardos (Ca2+ dependent) K+ channel blockers inhibit efflux of K+ and H2O from cell --> prevents dehydration of RBCs & reduce polymerization of HbS
428
Disulfiram
Used for recovering alcoholics Causes acetaldehyde accumulation --> bad side effects everytime someone consumes alcohol
429
Metronidazole
Trichomonas vaginitis & bacterial vaginosis Metronidazole + alcohol = acetaldehyde accumulation (bad side effects) b/c metronidazole inhibits alcohol oxidizing enzymes
430
What drug can cause atrialization of right ventricle?
Lithium --> Ebstein's anomaly in infants in utero Apical displacement of tricuspid valve leaflets --> decrease volume of RV (atrialization of RV) Lithium used to treat bipolar disease
431
Infant born w/ irritability, diarrhea, vomiting; could be due to withdrawal symptoms of what?
Narcotic use
432
Side effect of direct vasodilators? What are some examples of direct vasodilators? What drugs are given in combination to decrease side effects?
Hydralazine Minoxidil Used for HTN Significant arterial vasodilation can cause REFLEX sympathetic activation (sodium and fluid retention to bring BP up) --> tachycardia and edema Give sympatholytics & diuretics to help w/ side effects
433
Persistent cough & angioedema - side effect of what Rx?
ACE inhibitor
434
Failure of alveolar air to equilibrate w/ venous blood gases; possible cause?
Poor perfusion -- no exchange btwn alveoli & vessels (normal equilibration is pO2 ~100mmHg and pCO2 ~40mmHg)
435
Significant side effects of antihyperlipidemic medications
Statins - hepatoxicity, muscle toxicity Fibrates - muscle (esp combined w/ statins); gallstones Bile acid sequestrants - DECREASE absorption of digoxin, warfarin, fat-soluble vitamins; nausea, bloating, cramping Niacin - hepatotoxicity; flushing, warmth, pruritus Ezetimibe - hepatotoxicity (esp. with statins)
436
Blood supply of spleen
Splenic artery from celiac trunk (foregut) BUT spleen is MESODERM-derived foregut: esophagus --> 2nd part of duodenum, liver, gallbladder, and small portion of pancreas
437
Nesiritide
BNP (brain natriuretic peptide) dilates arteriole & veins - promotes diuresis usually released in pts. w/ systolic dysfunction in CHF (increased heart volume in heart that can't pump out a lot of blood --> increased stretching triggers ANP from atria or BNP from brain to be released to decrease volume)
438
Bradykinin relationship to adrenergic and renin-AT-aldosterone system
Bradykinin produced by kidneys when adrenergics and renin-AT-aldosterone system activated Constricts veins, dilates arterioles --> increase renal perfusion ANGIOEDEMA
439
Ranitidine
Proton pump inhibitor Ranitidine superior to H2 blockers for treatment of peptic ulcer disease
440
Misoprostol
PGE1 analog Prevents NSAID-induced ulcer disease
441
Liver function tests should be monitored for what drugs?
Carbamazepine Isoniazid (can cause full-blown hepatitis)
442
What drugs affect TSH and T3/T4 levels (levels should be monitored?)
Lithium - hypothyroidism Amiodarone - hypothyroidism
443
Entacapone
COMT inhibitor - increase levodopa bioavailability by inhibiting peripheral methylation (so levodopa can't be degraded peripherally --> more levodopa in brain); Entacapone HAS to be used in combination w/ levodopa; Entacapone by itself has no effects Tolcapone - COMT inhibitor that inhibits both peripheral and central methylation -- NOT used as often because of hepatotoxicity
444
COMT inhibitor: what does it stand for?
Catechol-O-methyltransferase inhibitor No peripheral methylation
445
What does Carbidopa do when used in conjunction w/ levodopa?
Carbidopa is a peripheral dopa decarboxylase inhibitor
446
How is selegiline different from levodopa?
Selegiline is a MAO-B inhibitor --> decrease central dopamine degradation Levodopa + carbidopa --> dopamine precursor Entacapone is a COMT inhibitor --> increase bioavailability of levodopa in brain (HAS TO BE USED in combination w/ levodopa)
447
Amantadine: indications
Anti-influenza antiviral ALSO used to enhance effects of endogenous dopamine (increase synthesis, release, re-uptake of dopamine)
448
Dopamine agonists (4)
Bromocriptine Pergolide Pramipexole Ropinerole stimulate dopamine receptors (D2 receptors)
449
What drugs are used to treat drug-induced Parkinson's disease? What is the MOA of these drugs?
Trihexyphenidyl Benztropine Inhibit central muscarinic receptors Pts. w/ tremor as predominant symptom respond best
450
Ergonovine: MOA
Ergonovine = ergot alkaloid --> constrict smooth muscle via alpha-adrenergic and serotonergic receptors
451
Ergonovine test - what disease does it diagnose?
Prinzmetal's angina Coronary vasospasm --> transient transmural ischemia --> ST segment elevation (& chest pain due to ischemia)
452
Cancer drug toxicities: 1. Vincristine 2. Bleomycin 3. Doxorubicin 4. Cyclophosphamide 5. Mercaptopurine 6. Methotrexate
1. Vincristine - inhibit microtubule polymerization (M phase) -- NEUROTOXIC (finger numbness/tingling) 2. Bleomycin - PULMONARY FIBROSIS (dry cough + exertional dyspnea); flagellate skin discoloration 3. Doxorubicin - CHF 4. Cyclophosphamide - hemorrhagic cystitis 5. Mercaptopurine (S-phase): abdominal pain/jaundice/cholestasis 6. Methotrexate (for rheumatoid arthritis): cirrhosis
453
Difference btwn actions of SMX and Trimethoprim/Pyrimethamine
SMX: inhibits dihydropteroate synthase -- inhibits DHF acid synthesis TMP/Pyrimethamine: inhibits DHF reductase -- inhibits THF acid synthesis
454
Bacitracin: MOA
Inhibit mucopeptide transfer into growing cell wall --> inhibit cell wall synthesis
455
What drugs inhibit HDF reductase?
TMP Methotrexate Pyrimethamine Inhibit DHF reductase --> inhibit THF acid formation
456
What part of cell cycle does Methotrexate inhibit?
S phase (can't synthesize purine and thymidylic acid)
457
Pyrimethamine: indications
Antimalarial Toxoplasmosis Inhibits DHF acid reductase
458
Drugs that cause sulfa allergies (7)
``` Celecoxib Furosemide Thiazide TMP-SMX Sulfasalazine Sulfonylureas Acetazolamide ```
459
Potassium citrate is prescribed as prophylaxis to what?
Calcium stones in urine Citrate binds free Ca2+
460
Calcium oxalate crystal vs. Calcium phosphate (struvite) crystals
Calcium oxalate - requires acidic pH Calcium phosphate (struvite) - requires alkaline pH
461
AZT (Zidovudine): MOA
NRTI (nucleoside reverse transcriptase inhibitor) competes w/ RT --> incorporated into viral genome as THYMIDINE analog has azido group in place of -OH group normally found at 3' end of thymidine LACK of free 3' -OH prevents new nucleotides from being added in replicating DNA --> PREVENTS DNA CHAIN ELONGATION