Exam 4: Drugs 1 Flashcards
Heparin (Unfractionated)
Indirect thrombin inhibitor; interacts with BOTH antithrombin and Xa
Produces more antithrombin = blocking thrombin from being produced
Reversal for heparin
Protamine sulfate
3 Indirect Thrombin Inhibitors
- Heparin
- LMW Heparin
- Fondapurinux
LMW Heparin
More purified; more specific for Xa
-parin drugs
Protamine sulfate = less effective
Fondapurinux
Pentasaccharide (same found in heparin)
Only activates antithrombin
No effect from protamine sulfate
2 Direct thrombin inhibitors
- Lepirudin (Hirudin)
- Argatroban (Pradaxa)
Indirect thrombin inhibitors MOA
Work on proteins that activate thrombin; usually Xa and antithrombin
Direct Thrombin inhibitors MOA
Bind to active sites on thrombin itself to prevent fibrin clot from forming
Lepirudin (Hirudin)
Produced from leeches and recombinant; prevents compartment syndrome
Argatroban/Dabigatran (Pradaxa)
produced from biological sources
3 Coumarin anticoagulants
- Warfarin (Coumadin)
- Ribaroxaban (Xarelto)
- Apixaban (Eliquis)
Warfarin
Oral anticoag; blocks vitamin K reductase = preventing gamma carboxylation of glutamate residues
Which clotting factors does warfarin block?
2, 7, 9, 10
Rivaroxaban (Xarelto) and Apixaban (eliquis)
Block vitamin K reductase; specific for Xa; less problems w/ bleeding out
No reversal
3 fibrinolytics
- tPA
- Streptokinase
- Urokinase
tPA
tissue plasminogen activators; produced in spot of damage
Streptokinase
synthesized by streptococci
Urokinase
synthesized by kidney
Fibrinolytics
Encourage plasmin formation from plasminogen = lyses thrombi
3 antiplatelets
- ASA
- Clopidogrel (Plavix)
- Abciximab
Aspirin
COX 1 selective; prevents activation of arachidonic acid cascade = less TXA2 produced
Clopidogrel (Plavix)
irreversibly inhibits ADP receptor on plts; reduces plt aggregation
used w/ angioplasty/stent placements
Abciximab
target IIb/IIIa glycoproteins that cause plt aggregation; blocks receptors and block aggregation
3 drugs used in bleeding disorders
- Vitamin K
- FFP
- Desmopressin
2 fibrinolytic inhibitors
- Aminocaproic acid
- Tranexamic acid (TXA2)
4 types of insulin
- Rapid-acting
- Short-acting (regular)
- Intermediate-acting
- Long acting
3 rapid-acting insulin drugs
- Lispro
- Aspart.
- Glulisine
2 short-acting insulin drugs
- Novolin
- Humulin
1 intermediate acting insulin drug
- Neutral protamine hagedorn
2 long-acting insulin drugs
- Glargine
- Detemir
Biguanides (1 drug)
2 guanines joined end to end
Metformin
Metformin
First line therapy for non-insulin dependent DM
2 insulin secretagogues
- Sulfonylurea (1st and 2nd generation)2.
- Thiazolidinediones
Sulfonylureas
bind to potassium channels and release more insulin via calcium coming into the cell and binding to cells containing insulin and releasing more insulin
Thazolidinediones
Inc. insulin resistance; inc. insulin signal transduction via PPAR pathway
Bind to receptors and inc. likelihood that cells respond better to insulin
Alpha-glucosidase inhibitors (1)
- Acarbose
Bile acid binding resin (BABR) (work in 2 different disease pathways)
Diabetes & dyslipidemia
Large resin gloop that prevents glucose from being reabsorbed by blocking it;
Amylin analog
amylin is released by beta cells and suppresses glucagon release (decreases circulating glucose); taken w/ insulin usually
Incretin-based therapies (3)
- Semaglutide
- Sitagliptin
- Gliflozin
Semaglutide
Inc. GLP-1; stimulates insulin release & inhibits glucagon release
Sitagliptin
Blocks DDP-4 (which breaks down GLP-1); stimulates more insulin release
Gliflozin
SGLT-2 inhibitors
-flozin drugs
prevent glucose uptake in PCT
Dyslipidemia drugs (2 major ones)
- Statins
- Niacin
Fibrates (1)
- Gemfibrozil
Inhibitors of intestinal Sterol absorption
- Ezetimibe
PCSK9 Inhibitors
Evolocumab
MAIN NSAID
Aspirin
COX 2 selective inhibitors (2)
- Celecoxib
- Meloxicam
Non-selective COX inhibitors (6)
- Diclofenac
- Ibuprofen
- Indomethacin
- Ketorolac
- Acetaminophen
- Glucocorticoids
DMARDS (disease modifying anti-rheumatic drugs) (3)
- Abatacept
- Rituximab
- Adalimumab
Abatacept
blocks t cell activation
Rituximab
depletes b-lymphocytes
Adalimumab
anti-TNF alpha
Phenanthrenes (opioids) (5/6)
- Morphine
- Dilaudid
- Codeine
- Oxycodone
- Percadan/Percocet
Phenylheptylamines (1)
Methadone
Phenylpiperidines (3)
- Fentanyl
- Meperidine (demerol)
- Tramadol
Buprenorphine
opioid abuse; partial opioid agonist
Butorphanol
post-op shivering; partial opioid agonist
Dextromethorphan
antitussive; weak opioid agonist
Derivatives of morphine (3)
- Naloxone
- Naltrexone
- Naloxegol
Inhibition of cell wall synthesis (6)
- Penicillin
- Ampicillin
- Amoxicillin
- Cephalosporin
- Carbepenem
- Vanco
Disruption of cell membrane (2)
- Polymyxin
- Daptomycin
Inhibition of protein synthesis (2 groups)
Tetracyclines and Macrolides
Macrolides (3)
- Erythromycin
- Azithromycin
- Neomycin
Erythromycin
prototype drug
azithromycin
semi-synthetic derivatable
neomycin
triple antibiotic; topical
inhibition of nuclein acid synthesis (2)
- Rifamycin
- Ciprofloxacin (cipro)
Inhibition of folic acid synthesis
Sulfonamides
Ketoconazole
antifungal; cream for cell membrane
Lamisil
topical dermatophytes
Antiprotazoan agents (2)
- Hydroxychloroquine
- Metronidazole
Hydoxychloroquine
malaria
Metronidazole
giardia, trichomonas
Parasidic worms (3)
- niclosamide
- Ivermectin
- Permethrin
Nicolsamide
tapeworms
Ivermectin
river blindness roundworm; vet care
COVID drug?
permethrin
lice
Antivirals (5)
- Acyclovir
- Azidothymidine (AZT)
- Lamivudine
- Cabotegrovir
- Interferon
Flu drugs (3)
- Oseltamivir phosphate (Tamiflu)
- Zanamivir (Relenza)
- Baloxivir marboxil (Xofluza)
COVID drugs (4)
- Paxlovid
- Remdesivir
- COVID Mabs
- Dexamethasone