Master Exam 2 Drugs

Valacylclovir

prodrug of acyclovir, anti-herpesvirus drug, viral thymidine kinase activates a nucleoside analog » analog incorporates into DNA and prevents elongation

oseltamivir

neuraminidase inhibitor (inflenza A/B), prevents virion release by budding, effective only if given early

baloxavir

cap-dependent endonuclease inhibitor, inhibits mRNA transcription, shortens symptoms by a day

nirmatre/ritonavir

paxlovid ~ COVID19 treatment, MPro inhibitor (nirmatrelvir) inhibit CYP3A4 (ritonavir, drug interaction potential)

Molnupiravir

tautomerization between 2 DNA isomers » leads to mutations in RNA with error in viral replication

molecular shape can cause contraindication in pregnancy, PT must finish treatment and isolate

cyclophosphamide

cytotoxic drug, nitrogen mustard alkalyting agent, react and crosslink DNA, can cause cell arrest & malfunctioning of DNA coding

doxorubicin

cytotoxic drug, anthracycline nonspecific phase (strong G2), intercalates DNA

etoposide

cytotoxic drug, topoisomerase inhibitor, permanent DNA strand breakage

paclitaxel

cytotoxic drug, microtubule/mitosis inhibitor (M phase specific)

imatinib

kinase inhibitor, prevents ATP from binding BCR-ABL » lowers proliferation signaling

Y90 Ibritumomab

anti-CD20 antibody » attacks B cell lymphoma

Bevacizumab

antibody binds to VEGF » prevents blood vessel supply to tumor

Pembrolizumab

antibody blocks PD1 on tumor cells » allows T cell activation to kill tumor

lidocane

standard local anesthetic (1-2 hr duration)

epinephrine

vasoconstrictor local anesthetic, less drug in systemic circulation (stays at infiltration site), used in PTs with CVD risk

succinylcholine

relaxant that depolarizes and causes NAChR activation, used for intubations

rocurinium

nondepolarizing neuromuscular blocker (relaxant), used for surgery with other general anesthetics

Aspirin

aceetylates COX1 and 2, irreversible inhibitor, analgesic, antipyretic, antithrombotic

ibuprofen

inhibits COX, prefers COX1

celecoxib

inhibits COX2 » increased stroke or M1 cardiovascular risk

acetaminophen (tylenol)

weak COX1 and 2 inhibitor because of concentration of peroxide at inflammation site, activates TRPV1 and CB1 receptors, not anti-inflammatory

toxicity at 7-10g » flu like symptoms

morphine

opioid prototype drug

oxycodone

lower efficacy and bioavailability than morphine, oxycontin is a version that contributed to opioid epidemic

codeine

low efficacy opioid, prodrug susceptible to CYP2D6 pharmacogenetics

fentanyl

fast-acting, potent, short duration opioid

naloxone

narcan, treat opioid overdse

Clopidogrel

anti-platelet drug, ADP receptor antagonist that blocks P2Y12 in platelets

bruising and bleeding

aspirin

anti-platelet drug, TXA2 synthesis inhibitor that inhibits COX1

gi effects

warfarin

anticoagulant drug, inhibits VKORC1 = no VitK activation » no clotting factor synthesis

metabolized by CYP2C9 » bleeding risk with genetic variation

rivaroxaban

anticoagulatnt drug, inhibit factor Xa (clotting), DOAC

heparin

anticoagulant drug, activates antithrombin » inhibits thrombin and Xa (immediate anticoagulant effect)

Sacubitril/Valstartan

block neprilysin and angiotensin II to angiotensin receptor conversion » more bradykinin and angiotensin II » increases vasodilation

Digoxin

• block Na/IK ATP ase » less Ca removal, more Ca binding to troponin

• increase vagal firing, PSNS

atorvastatin

high intensity statin, inhibit HMG CoA reductase » lower cholesterol by increasing LDL-R

increased liver enzymes, myopathy, T2 diabetes risk

alirocumab

inhibit PCSK9 » more LDL clearance

ezetimibe

block intestinal cholesterol absorption » more LDL clearance, lower absorption of dietary and biliary cholesterol

bempedoic acid

inhibit ATP citrate lyase » lowers cholesterol precursor in liver

Furosemide

Loop diuretic, block NKCC2 transport in ascending limb, hypokalemia

Hydrochlorothiazide (HCTZ)

thiazide diuretic, block NCC in distal tubule, hypokalemia

amiloride

K+ sparing diuretic, block Na+ channels in collecting duct, hyperkalemia

spironolactone

K+ sparing diuretic, block aldosterone receptor in collecting duct, hyperkalemia, anti-androgen effs.

lisinopril

renin-angiotensin drug, ACE inhibitor » dry cough

losartan

renin-angiotensin drug, angiotensin receptor blocker (ARB),

amlodipine

DHP selective for vessels

verapamil

non-DHP, blocks Ca2+ channels