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Drugs Step 1 > Top 100 Drugs > Flashcards

Top 100 Drugs Flashcards

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
Q

Mechanism of -tide?

A

GLP-1 analog - increase insulin
- decrease glucagon
SE: pancreatitis

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26
Q

Mechanism of -gliptin?

A

DPP-4 inhibitors - increase insulin

- decrease glucagon

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27
Q

Mechanism of first line therapy in T2DM?

A

Metformin - a biguanide
- decrease gluconeogenesis
- increase glycolysis
- increase peripheral glucose uptake (increase insulin sensitivity)
SE: Lactic acidosis - watch creatinine levels

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28
Q

Binds PPAR-gamma a nuclear transcription regulator to do what?

A

-glitazone (TZD)
Increase insulin sensitivity in peripheral tissue
SE: weight gain

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29
Q

Mechanism of acarbose or miglitol?

A

Inhibit intestinal brush border a-glucosidases

- delayed carb hydrolysis & glucose absorption

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30
Q

H2 Blockers

A 
Cimetidine: inhibitor of P450
Ranitidine
Famotidine
Nizatidine
Take H2 blockers before you -dine
Treat Peptic Ulcer, gastritis, mild reflux
31
Q

Mechanism of drug to treat Zollinger-Ellison & GERD?

A

Irreversibly inhibit H/K ATPase in stomach parietal cells

32
Q

Bind to ulcer base, provide physical protection

Promote HCO3 secretion

A

Treat active duodenal ulcers - increase ulcer healing

Treat Travelers’ Diarrhea

33
Q

Mechanism of drug to prevent NSAID-induced peptic ulcers?

A

Misoprostol

  • PGE1 analog = increase mucous = barrier
  • decrease acid production

NSAIDs block PGE1 production

34
Q

Treat acute variceal bleeds, VIPoma, and??

A

Octreotide - long acting somatostatin analog

  • also treat Acromegaly
  • also treat carcinoid tumors
35
Q

Treat Ulcerative colitis & Crohn disease?

A 
Sulfasalazine
 - combo of antibacterial sulfapyridine
 - and anti-inflammatory 5-aminosalicylic acid
**activated by colonic bacteria
SE: oligospermia
36
Q

Dance until 3am and then STOP

A

Ondansetron
- 5-HT3 antagonist = central acting antiemetic
- decreases Vagal stimulation
SE: QT prolongation

37
Q 
Treat Gastroparesis (delayed gastric emptying)
 - food remains in stomach for long time
A

Metoclopramide - D2 antagonist
- increases resting tone & contractility
SE: Parkinson, tardive dyskinesia, interact w/ digoxin

38
Q

Weight loss drug to decrease breakdown and absorption of dietary fats

A

Orlistat

SE: decreased fat soluble vitamins

39
Q

Cross-link DNA at guanine

- treat tumors

A

Cyclophosphamide
SE: myelosuppression
hemorrhagic cystitis - less w/ mesna

40
Q

Paclitaxel - taxols

A

Hyperstablize microtubules in M phase
- mitotic spindle can’t break down
SE: myelosuppression

41
Q

Vinca alkaloid, bind beta-tubulin

  • inhibit polymerization into microtubules
  • prevent mitotic spindle formation
A

Vincristine / Vinblastine
- treat tumors, leukemias, Hodgkin & Non-Hodgkin
SE: neurotoxic / bone marrow suppression

42
Q

Rituximab

A

Monoclonal antibody vs. CD20 – B-cell cancers

SE: increased risk PML

43
Q

SERMS: block binding to ER + cells

A

Tamoxifen - breast CA only; SE endometrial CA

Raloxifen - prevent osteoporosis, less endometrial

44
Q

Mechanism of drug treat RA & OA

A

Celecoxib: reversibly inhibit COX-2 – selective

  • less effect on GI lining
  • spares platelet functioning
45
Q

SE of NSAIDs?

A

Interstitial nephritis
Gastric Ulcer
Renal ischemia (block prostaglandins)

46
Q

Mechanism of drug to treat Osteoporosis or Paget of Bone?

A

Pyrophosphate analog, bind hydroxyapatite in bone
- inhibit osteoclast activity
Bisphosphonates: alendronate

47
Q

Two drugs, inhibit Xanthine Oxidase

A

Allopurinol: increases 6-MP/azathioprine

Febuxostat

48
Q

Treat gout - mechanism?

A

Colchicine

  • bind & stabilize tubulin
  • inhibit microtubule polymerization
  • impairs neutrophil chemotaxis & degranulation
49
Q

Predisposes to infection (TB)

Treat RA, ankyl, psoriasis, IBD

A

Etanercept: TNF decoy receptor

Infliximab/adalimumab: anti-TNF-alpha - dues IBD too

50
Q

Treat Glaucoma

A 
Epinephrine - a1 agonist
Brimonidine - a2 agonist
Timolol - BB
Acetazolamide
All lower aqueous humor synthesis
51
Q

Mechanism of opioid analgesics

A

Morphine, fentanyl, Loperamide, Diphenoxylate
- open K+ channels & close Ca++ channels
- decrease synaptic transmission
Inhibit release ACh, NE, 5-HT, Glutamate, Substance P

52
Q

Tramadol

A

Weak opioid agonist
Inhibit 5-HT and NE reuptake
Tram it all w/ Tramadol = works on multiple transmitters
SE: decrease seizure threshold

53
Q

Treat absence seizure by what mechanism?

A

Ethosuximide
- block thalamic T-type Ca++ channels

SE: EFGHIJ Itch, Stevens-Johnson

54
Q

Epilepsy drugs that increase Na+ channel inactivation?

A 
Phenytoin
Carbamazepine
Topiramate
Lamotrigine
Valproic Acid - also increase GABA
55
Q

Epilepsy drugs increase GABA?

A 
Valproic Acid - also increase Na+ inactivation
Tiagabine
Viagabatrin
Phenobarbital
Benzodiazepines
Gabapentin
56
Q

Duration vs. Frequency of Cl- channel opening

A

Barbiturates: increase duration
Benzodiazepines: increase frequency

57
Q

Short acting BDZ’s?

A 
ATOM
 - Alprazolam
 - Triazolam
 - Oxazepam
 - Midazolam
Higher potential for addiction
58
Q

Side Effects of Inhaled Anesthetics

A

Halothane - liver
Methoxyflurane - kidney
Enflurane - proconvulsant
N20 - expansion of trapped gas in a body cavity
All + Succinylcholine = malignant hyperthermia

59
Q

PCP analog that causes dissociative anesthetic

A

Ketamine

- increases cerebral blood flow (not a good thing)

60
Q

Most common drug for endoscopy?

A

Midazolam

- severe postop respiratory depression

61
Q

Succinylcholine

A

Phase I: prolonged depolarization, no antidote
Phase II: ACh receptors available but desensitized
- antidote = cholinesterase inhibitors

62
Q

Activates ______ receptors at spinal cord level

- get skeletal muscle relaxation

A

Activates GABA-b

Baclofen

63
Q

Dopamine agonist

A

Bromocriptine - ergot

64
Q

Dopamine agonist - non-ergot

A

Pramipexole

Ropinirole

65
Q

Levodopa

A

Give with carbidopa - block peripheral conversion of L-DOPA to dopamine
- inhibits Dopa decarboxylase

66
Q

Entacapone / tolcapone

A

Prevent peripheral L-dopa degradation to 3-O-methyldopa by inhibiting COMT

67
Q

Block breakdown of dopamine by?

A

Selectively inhibiting MAO-B

68
Q

NMDA receptor antagonist - treat Alzheimer

A

Memantine

69
Q

Inhibit VMAT - treat?

A

Reserpine

- treat Huntingeon

70
Q

Sumatriptan

A

5-HT 1B/1D agonist
- treat acute migraine
- treat cluster headache
SE: contraindicated w/ CAD and Prinzmetal

71
Q

Gram Positive Antibiotic w/ MAOi activity

- cause what with what?

A

Linezolid

- cause serotonin syndrome w/ SSRI (Paroxetine)

72
Q

Treat ADHD drug mechanism?

A 
Want to increase NE & Dopamine
Stimulant drugs
 - methylphenidate
 - amphetamines
Block NE & D reuptake in prefrontal cortex
73
Q

Treat seizure and bipolar?

A

Valproic acid

Drugs Step 1 (5 decks)

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