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Drugs Step 1 > Top 100 Drugs > Flashcards

Top 100 Drugs Flashcards

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1
Q

Inhibit IMP dehydrogenase

A

Mycophenolate & Ribavirin

- should take IMP —– GMP

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2
Q

Hydroxyurea

A

Inhibits ribonucleotide reductase

  • should take UDP to dUDP – then to dUMP
  • and finally to dTMP
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3
Q

Inhibit thymidylate synthase

A

5-Fluorouracil

- can’t convert dUMP to dTMP

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4
Q

Inhibit dihydrofolate reductase

A

Methotrexate, Trimethoprim, Pyrimethamine
- needed to recycle DHF to THF
- THF needed to convert dUMP to dTMP
Humans, Bacteria, Protozoa

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5
Q

6-Mercaptopurine & Azathioprine

A

Inhibit Purine De Novo Pathway
- blocks nucleotide synthesis
Treat: RA, Crohn, transplant rejection
SE: Leukopenia + Thrombocytopenia + Anemia
6-MP is degraded by XO which is blocked by Allopurinol

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6
Q

Fluoroquinolones

A

Inhibit prokaryote Topoisomerase II (DNA gyrase) & IV
- can’t create single/double stranded breaks in helix
- can’t add/relieve supercoil
- can’t unwind and duplicate
Broad-spectrum antibiotic

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7
Q

Block T-cell activation

Prevents IL-2 transcription

A

Cyclosporin - calcineurin inhibitor - cyclophilin

Tacrolimus - calcineurin ihhibitor FK506

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8
Q

Block T-cell activation
Block B-cell differentiation
Prevents response to IL-2

A

Sirolimus / Rampamycin

- mTOR inhibitor

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9
Q

Inhibit NFkB

Suppress T and B cell function by…

A

…by suppression of transcription of many cytokines
Glucocorticoids
SE: hyperglycemia, osteoporosis, cushing

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10
Q

Rifampin mech

A

Inhibits RNA polymerase in prokaryotes

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11
Q

Amiadarone vs. Sotalol

A 
Amiodarone - check PFT, LFT, TFT (no risk TdP)
 - lipophilic has class I-IV effects        (gray skin)
Sotalol & Ibutilide = TdP
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12
Q

Decrease SA & AV node activity by decrease cAMP and decrease Ca++ currents
Decrease slope of phase 4

A

Beta-blockers as antiarrhythmics

SE: mask signs hypoglycemia
unopposed a1 in pheo & cocaine toxicity
propranolol makes Prinzmetal worse

BB Overdose: give Glucagon

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13
Q

Mechanism of drug used to treat HF and Atrial Fibrillation

A

Direct inhibition of Na/K ATPase = + Inotropy
Indirect inhibition of Na/Ca exchanger
Stimulate Vagus – decrease HR
SE: Yellow vision, arrhythmias, HYPERkalemia

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14
Q

Activate PPAR-a to induce HDL synthesis and decrease VLDL

A

Fibrates
- see decrease in TG
- inhibit chol 7a-hydroxylase = RLS bile acid synth
SE: Myopathy, Cholesterol Gallstones

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15
Q

Inhibit lipolysis (HSL) in adipose tissue and reduce hepatic VLDL synthesis

A

Niacin (B3)
- increases HDL
SE: flushing (give NSAID), hyperuricemia (Gout)
Avoid alcohol

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16
Q

Inhibit conversion of HMB-CoA to mevalonate – a cholesterol percursor. Increase surface LDL receptors

A

Statins / HMG-CoA Reductase inhibitors
SE: myopathy & hepatotoxicity
(worse = myositis rhabdomyolysis)

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17
Q

Vasodilate arteries by increasing cGMP = smooth muscle relaxation = decrease afterload

A

Hydralazine
Any vasodilator may cause reflex tacky
SHIPP

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18
Q

Drugs for Hypertensive Emergency

A

Fenoldopam = D1 agonist - vasodilation
Nitroprusside = increase cGMP, direct release of NO
(ssscyanide toxicity, treat w/ thiosulfate)

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19
Q

Mechanism of the drug used to decrease preload?

A

Nitrates: vasodilate by increase NO, increase cGMP = SM relax
Monday Disease: tolerance for dilation during week, get reflex tachycardia, dizzy, HA upon re-exposure

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20
Q

Treat HTN in:

  • Diabetic
  • HF
  • Primary/essential HTN
A

DM = ACE inhibitor/ARB or CCB, thiazide, BB

HF = Diuretic, ACE/ARB, BB, aldosterone antagonist

Primary = Thiazide, ACE, ARB, CCB (-dipine)

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21
Q

Long-Acting Insulin

A

Detemir
Glargine
NPH is intermediate

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22
Q

Mechanism of zide/ride/ride & other one?

A

Close K+ channel = depolarization
- insulin release via increased Ca++
SE: hypoglycemia

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23
Q

Mechanism of drug(s) used to treat Hyperthyroidism?

SE?

A

Propylthiouracil, methimazole
- block thyroid peroxidase = block oxidation & organification
Propyl also peripheral conversion T4 – T3 (5-deiodinase)
SE: agranulocytosis

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24
Q

Side effects of drug used to treat Hypothyroidism?

A

Levothyroxine T4

- tachycardia, heat intolerance, arrhythmias

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25
Mechanism of -tide?
GLP-1 analog - increase insulin - decrease glucagon SE: pancreatitis
26
Mechanism of -gliptin?
DPP-4 inhibitors - increase insulin | - decrease glucagon
27
Mechanism of first line therapy in T2DM?
Metformin - a biguanide - decrease gluconeogenesis - increase glycolysis - increase peripheral glucose uptake (increase insulin sensitivity) SE: Lactic acidosis - watch creatinine levels
28
Binds PPAR-gamma a nuclear transcription regulator to do what?
-glitazone (TZD) Increase insulin sensitivity in peripheral tissue SE: weight gain
29
Mechanism of acarbose or miglitol?
Inhibit intestinal brush border a-glucosidases | - delayed carb hydrolysis & glucose absorption
30
H2 Blockers
``` Cimetidine: inhibitor of P450 Ranitidine Famotidine Nizatidine Take H2 blockers before you -dine Treat Peptic Ulcer, gastritis, mild reflux ```
31
Mechanism of drug to treat Zollinger-Ellison & GERD?
Irreversibly inhibit H/K ATPase in stomach parietal cells
32
Bind to ulcer base, provide physical protection | Promote HCO3 secretion
Treat active duodenal ulcers - increase ulcer healing | Treat Travelers' Diarrhea
33
Mechanism of drug to prevent NSAID-induced peptic ulcers?
Misoprostol - PGE1 analog = increase mucous = barrier - decrease acid production NSAIDs block PGE1 production
34
Treat acute variceal bleeds, VIPoma, and??
Octreotide - long acting somatostatin analog - also treat Acromegaly - also treat carcinoid tumors
35
Treat Ulcerative colitis & Crohn disease?
``` Sulfasalazine - combo of antibacterial sulfapyridine - and anti-inflammatory 5-aminosalicylic acid **activated by colonic bacteria SE: oligospermia ```
36
Dance until 3am and then STOP
Ondansetron - 5-HT3 antagonist = central acting antiemetic - decreases Vagal stimulation SE: QT prolongation
37
``` Treat Gastroparesis (delayed gastric emptying) - food remains in stomach for long time ```
Metoclopramide - D2 antagonist - increases resting tone & contractility SE: Parkinson, tardive dyskinesia, interact w/ digoxin
38
Weight loss drug to decrease breakdown and absorption of dietary fats
Orlistat | SE: decreased fat soluble vitamins
39
Cross-link DNA at guanine | - treat tumors
Cyclophosphamide SE: myelosuppression hemorrhagic cystitis - less w/ mesna
40
Paclitaxel - taxols
Hyperstablize microtubules in M phase - mitotic spindle can't break down SE: myelosuppression
41
Vinca alkaloid, bind beta-tubulin - inhibit polymerization into microtubules - prevent mitotic spindle formation
Vincristine / Vinblastine - treat tumors, leukemias, Hodgkin & Non-Hodgkin SE: neurotoxic / bone marrow suppression
42
Rituximab
Monoclonal antibody vs. CD20 -- B-cell cancers | SE: increased risk PML
43
SERMS: block binding to ER + cells
Tamoxifen - breast CA only; SE endometrial CA | Raloxifen - prevent osteoporosis, less endometrial
44
Mechanism of drug treat RA & OA
Celecoxib: reversibly inhibit COX-2 -- selective - less effect on GI lining - spares platelet functioning
45
SE of NSAIDs?
Interstitial nephritis Gastric Ulcer Renal ischemia (block prostaglandins)
46
Mechanism of drug to treat Osteoporosis or Paget of Bone?
Pyrophosphate analog, bind hydroxyapatite in bone - inhibit osteoclast activity Bisphosphonates: alendronate
47
Two drugs, inhibit Xanthine Oxidase
Allopurinol: increases 6-MP/azathioprine Febuxostat
48
Treat gout - mechanism?
Colchicine - bind & stabilize tubulin - inhibit microtubule polymerization - impairs neutrophil chemotaxis & degranulation
49
Predisposes to infection (TB) | Treat RA, ankyl, psoriasis, IBD
Etanercept: TNF decoy receptor | Infliximab/adalimumab: anti-TNF-alpha - dues IBD too
50
Treat Glaucoma
``` Epinephrine - a1 agonist Brimonidine - a2 agonist Timolol - BB Acetazolamide All lower aqueous humor synthesis ```
51
Mechanism of opioid analgesics
Morphine, fentanyl, Loperamide, Diphenoxylate - open K+ channels & close Ca++ channels - decrease synaptic transmission Inhibit release ACh, NE, 5-HT, Glutamate, Substance P
52
Tramadol
Weak opioid agonist Inhibit 5-HT and NE reuptake Tram it all w/ Tramadol = works on multiple transmitters SE: decrease seizure threshold
53
Treat absence seizure by what mechanism?
Ethosuximide - block thalamic T-type Ca++ channels SE: EFGHIJ Itch, Stevens-Johnson
54
Epilepsy drugs that increase Na+ channel inactivation?
``` Phenytoin Carbamazepine Topiramate Lamotrigine Valproic Acid - also increase GABA ```
55
Epilepsy drugs increase GABA?
``` Valproic Acid - also increase Na+ inactivation Tiagabine Viagabatrin Phenobarbital Benzodiazepines Gabapentin ```
56
Duration vs. Frequency of Cl- channel opening
Barbiturates: increase duration Benzodiazepines: increase frequency
57
Short acting BDZ's?
``` ATOM - Alprazolam - Triazolam - Oxazepam - Midazolam Higher potential for addiction ```
58
Side Effects of Inhaled Anesthetics
Halothane - liver Methoxyflurane - kidney Enflurane - proconvulsant N20 - expansion of trapped gas in a body cavity All + Succinylcholine = malignant hyperthermia
59
PCP analog that causes dissociative anesthetic
Ketamine | - increases cerebral blood flow (not a good thing)
60
Most common drug for endoscopy?
Midazolam | - severe postop respiratory depression
61
Succinylcholine
Phase I: prolonged depolarization, no antidote Phase II: ACh receptors available but desensitized - antidote = cholinesterase inhibitors
62
Activates ______ receptors at spinal cord level | - get skeletal muscle relaxation
Activates GABA-b | Baclofen
63
Dopamine agonist
Bromocriptine - ergot
64
Dopamine agonist - non-ergot
Pramipexole | Ropinirole
65
Levodopa
Give with carbidopa - block peripheral conversion of L-DOPA to dopamine - inhibits Dopa decarboxylase
66
Entacapone / tolcapone
Prevent peripheral L-dopa degradation to 3-O-methyldopa by inhibiting COMT
67
Block breakdown of dopamine by?
Selectively inhibiting MAO-B
68
NMDA receptor antagonist - treat Alzheimer
Memantine
69
Inhibit VMAT - treat?
Reserpine | - treat Huntingeon
70
Sumatriptan
5-HT 1B/1D agonist - treat acute migraine - treat cluster headache SE: contraindicated w/ CAD and Prinzmetal
71
Gram Positive Antibiotic w/ MAOi activity | - cause what with what?
Linezolid | - cause serotonin syndrome w/ SSRI (Paroxetine)
72
Treat ADHD drug mechanism?
``` Want to increase NE & Dopamine Stimulant drugs - methylphenidate - amphetamines Block NE & D reuptake in prefrontal cortex ```
73
Treat seizure and bipolar?
Valproic acid

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