Top 100 Drugs Flashcards
Inhibit IMP dehydrogenase
Mycophenolate & Ribavirin
- should take IMP —– GMP
Hydroxyurea
Inhibits ribonucleotide reductase
- should take UDP to dUDP – then to dUMP
- and finally to dTMP
Inhibit thymidylate synthase
5-Fluorouracil
- can’t convert dUMP to dTMP
Inhibit dihydrofolate reductase
Methotrexate, Trimethoprim, Pyrimethamine
- needed to recycle DHF to THF
- THF needed to convert dUMP to dTMP
Humans, Bacteria, Protozoa
6-Mercaptopurine & Azathioprine
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
Fluoroquinolones
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
Block T-cell activation
Prevents IL-2 transcription
Cyclosporin - calcineurin inhibitor - cyclophilin
Tacrolimus - calcineurin ihhibitor FK506
Block T-cell activation
Block B-cell differentiation
Prevents response to IL-2
Sirolimus / Rampamycin
- mTOR inhibitor
Inhibit NFkB
Suppress T and B cell function by…
…by suppression of transcription of many cytokines
Glucocorticoids
SE: hyperglycemia, osteoporosis, cushing
Rifampin mech
Inhibits RNA polymerase in prokaryotes
Amiadarone vs. Sotalol
Amiodarone - check PFT, LFT, TFT (no risk TdP) - lipophilic has class I-IV effects (gray skin) Sotalol & Ibutilide = TdP
Decrease SA & AV node activity by decrease cAMP and decrease Ca++ currents
Decrease slope of phase 4
Beta-blockers as antiarrhythmics
SE: mask signs hypoglycemia
unopposed a1 in pheo & cocaine toxicity
propranolol makes Prinzmetal worse
BB Overdose: give Glucagon
Mechanism of drug used to treat HF and Atrial Fibrillation
Direct inhibition of Na/K ATPase = + Inotropy
Indirect inhibition of Na/Ca exchanger
Stimulate Vagus – decrease HR
SE: Yellow vision, arrhythmias, HYPERkalemia
Activate PPAR-a to induce HDL synthesis and decrease VLDL
Fibrates
- see decrease in TG
- inhibit chol 7a-hydroxylase = RLS bile acid synth
SE: Myopathy, Cholesterol Gallstones
Inhibit lipolysis (HSL) in adipose tissue and reduce hepatic VLDL synthesis
Niacin (B3)
- increases HDL
SE: flushing (give NSAID), hyperuricemia (Gout)
Avoid alcohol
Inhibit conversion of HMB-CoA to mevalonate – a cholesterol percursor. Increase surface LDL receptors
Statins / HMG-CoA Reductase inhibitors
SE: myopathy & hepatotoxicity
(worse = myositis rhabdomyolysis)
Vasodilate arteries by increasing cGMP = smooth muscle relaxation = decrease afterload
Hydralazine
Any vasodilator may cause reflex tacky
SHIPP
Drugs for Hypertensive Emergency
Fenoldopam = D1 agonist - vasodilation
Nitroprusside = increase cGMP, direct release of NO
(ssscyanide toxicity, treat w/ thiosulfate)
Mechanism of the drug used to decrease preload?
Nitrates: vasodilate by increase NO, increase cGMP = SM relax
Monday Disease: tolerance for dilation during week, get reflex tachycardia, dizzy, HA upon re-exposure
Treat HTN in:
- Diabetic
- HF
- Primary/essential HTN
DM = ACE inhibitor/ARB or CCB, thiazide, BB
HF = Diuretic, ACE/ARB, BB, aldosterone antagonist
Primary = Thiazide, ACE, ARB, CCB (-dipine)
Long-Acting Insulin
Detemir
Glargine
NPH is intermediate
Mechanism of zide/ride/ride & other one?
Close K+ channel = depolarization
- insulin release via increased Ca++
SE: hypoglycemia
Mechanism of drug(s) used to treat Hyperthyroidism?
SE?
Propylthiouracil, methimazole
- block thyroid peroxidase = block oxidation & organification
Propyl also peripheral conversion T4 – T3 (5-deiodinase)
SE: agranulocytosis
Side effects of drug used to treat Hypothyroidism?
Levothyroxine T4
- tachycardia, heat intolerance, arrhythmias
Mechanism of -tide?
GLP-1 analog - increase insulin
- decrease glucagon
SE: pancreatitis
Mechanism of -gliptin?
DPP-4 inhibitors - increase insulin
- decrease glucagon
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
Binds PPAR-gamma a nuclear transcription regulator to do what?
-glitazone (TZD)
Increase insulin sensitivity in peripheral tissue
SE: weight gain
Mechanism of acarbose or miglitol?
Inhibit intestinal brush border a-glucosidases
- delayed carb hydrolysis & glucose absorption
H2 Blockers
Cimetidine: inhibitor of P450 Ranitidine Famotidine Nizatidine Take H2 blockers before you -dine Treat Peptic Ulcer, gastritis, mild reflux
Mechanism of drug to treat Zollinger-Ellison & GERD?
Irreversibly inhibit H/K ATPase in stomach parietal cells
Bind to ulcer base, provide physical protection
Promote HCO3 secretion
Treat active duodenal ulcers - increase ulcer healing
Treat Travelers’ Diarrhea
Mechanism of drug to prevent NSAID-induced peptic ulcers?
Misoprostol
- PGE1 analog = increase mucous = barrier
- decrease acid production
NSAIDs block PGE1 production
Treat acute variceal bleeds, VIPoma, and??
Octreotide - long acting somatostatin analog
- also treat Acromegaly
- also treat carcinoid tumors
Treat Ulcerative colitis & Crohn disease?
Sulfasalazine - combo of antibacterial sulfapyridine - and anti-inflammatory 5-aminosalicylic acid **activated by colonic bacteria SE: oligospermia
Dance until 3am and then STOP
Ondansetron
- 5-HT3 antagonist = central acting antiemetic
- decreases Vagal stimulation
SE: QT prolongation
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
Weight loss drug to decrease breakdown and absorption of dietary fats
Orlistat
SE: decreased fat soluble vitamins
Cross-link DNA at guanine
- treat tumors
Cyclophosphamide
SE: myelosuppression
hemorrhagic cystitis - less w/ mesna
Paclitaxel - taxols
Hyperstablize microtubules in M phase
- mitotic spindle can’t break down
SE: myelosuppression
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
Rituximab
Monoclonal antibody vs. CD20 – B-cell cancers
SE: increased risk PML
SERMS: block binding to ER + cells
Tamoxifen - breast CA only; SE endometrial CA
Raloxifen - prevent osteoporosis, less endometrial
Mechanism of drug treat RA & OA
Celecoxib: reversibly inhibit COX-2 – selective
- less effect on GI lining
- spares platelet functioning
SE of NSAIDs?
Interstitial nephritis
Gastric Ulcer
Renal ischemia (block prostaglandins)
Mechanism of drug to treat Osteoporosis or Paget of Bone?
Pyrophosphate analog, bind hydroxyapatite in bone
- inhibit osteoclast activity
Bisphosphonates: alendronate
Two drugs, inhibit Xanthine Oxidase
Allopurinol: increases 6-MP/azathioprine
Febuxostat
Treat gout - mechanism?
Colchicine
- bind & stabilize tubulin
- inhibit microtubule polymerization
- impairs neutrophil chemotaxis & degranulation
Predisposes to infection (TB)
Treat RA, ankyl, psoriasis, IBD
Etanercept: TNF decoy receptor
Infliximab/adalimumab: anti-TNF-alpha - dues IBD too
Treat Glaucoma
Epinephrine - a1 agonist Brimonidine - a2 agonist Timolol - BB Acetazolamide All lower aqueous humor synthesis
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
Tramadol
Weak opioid agonist
Inhibit 5-HT and NE reuptake
Tram it all w/ Tramadol = works on multiple transmitters
SE: decrease seizure threshold
Treat absence seizure by what mechanism?
Ethosuximide
- block thalamic T-type Ca++ channels
SE: EFGHIJ Itch, Stevens-Johnson
Epilepsy drugs that increase Na+ channel inactivation?
Phenytoin Carbamazepine Topiramate Lamotrigine Valproic Acid - also increase GABA
Epilepsy drugs increase GABA?
Valproic Acid - also increase Na+ inactivation Tiagabine Viagabatrin Phenobarbital Benzodiazepines Gabapentin
Duration vs. Frequency of Cl- channel opening
Barbiturates: increase duration
Benzodiazepines: increase frequency
Short acting BDZ’s?
ATOM - Alprazolam - Triazolam - Oxazepam - Midazolam Higher potential for addiction
Side Effects of Inhaled Anesthetics
Halothane - liver
Methoxyflurane - kidney
Enflurane - proconvulsant
N20 - expansion of trapped gas in a body cavity
All + Succinylcholine = malignant hyperthermia
PCP analog that causes dissociative anesthetic
Ketamine
- increases cerebral blood flow (not a good thing)
Most common drug for endoscopy?
Midazolam
- severe postop respiratory depression
Succinylcholine
Phase I: prolonged depolarization, no antidote
Phase II: ACh receptors available but desensitized
- antidote = cholinesterase inhibitors
Activates ______ receptors at spinal cord level
- get skeletal muscle relaxation
Activates GABA-b
Baclofen
Dopamine agonist
Bromocriptine - ergot
Dopamine agonist - non-ergot
Pramipexole
Ropinirole
Levodopa
Give with carbidopa - block peripheral conversion of L-DOPA to dopamine
- inhibits Dopa decarboxylase
Entacapone / tolcapone
Prevent peripheral L-dopa degradation to 3-O-methyldopa by inhibiting COMT
Block breakdown of dopamine by?
Selectively inhibiting MAO-B
NMDA receptor antagonist - treat Alzheimer
Memantine
Inhibit VMAT - treat?
Reserpine
- treat Huntingeon
Sumatriptan
5-HT 1B/1D agonist
- treat acute migraine
- treat cluster headache
SE: contraindicated w/ CAD and Prinzmetal
Gram Positive Antibiotic w/ MAOi activity
- cause what with what?
Linezolid
- cause serotonin syndrome w/ SSRI (Paroxetine)
Treat ADHD drug mechanism?
Want to increase NE & Dopamine Stimulant drugs - methylphenidate - amphetamines Block NE & D reuptake in prefrontal cortex
Treat seizure and bipolar?
Valproic acid
