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MSK Therapeutics

MSK Exam 1 Drug info table

BrandGenericClassMOAUsesSide EffectsOther NotesRamsing Notes Unique
Tylenol Acetaminophen Analgesic COX inhibitor; inhibits prostoglandin synthesis in the CNS -Direct or indirect; peroxidases, NO synthase, endocannabinoids, TRPV ion channels, 5-HT reduces pain, fever Safe, low GI distress/ Nephro and hepatotoxic (*at high doses) Alternative to aspirin for viral infections (20 yo), Reye'syndrome -Plays a bigger role in the CNS and more selectivey for blocking COX-2 *weak anti-inflammatory *Know strucutre of APAP and NAPQI *CYP2E1 (induced by alcohol means more NAPQI *exhausting of GSH--> Hepatocytes (hepatotoxicity) Antidote: NAC (conjugate via -SH)
Motrin Ibuprofen *short acting (<6H) Propionic NSAID Reversible; non-selective COX inhibitor Inflammation, Pain, fever, anti-thrombotic Box warning: CV, GI, bleeding risk, edema *contains an alpha methyl (enhances anti-inflammatory activity) and a chrial carbon *racemic R to S-enantiomer (S has the activity)
Naprosyn, Anaprox, Anaprox DS (RX); Aleve (OTC) Naproxen *long acting (>6H) Propionic NSAID Reversible; non-selective COX inhibitor Inflammation, Pain, fever, anti-thrombotic Box warning: CV, GI, bleeding risk, edema Naproxen has longer half-life in comparison to the other Propionic NSAIDS (t1/2: 12-15 hours) *contains an alpha methyl (enhances anti-inflammatory activity) and a chrial carbon *racemic R to S-enantiomer (S has the activity) *only drug marketed as S-enantiomer
Indocin Indomethacin *short acting (<6H) Acetic Acid NSAID Derivative Reversible; non-selective COX inhibitor *Ramsinghani--> "pseudoirreversible inhibtion of COX" (*CH3 group) Inflammation, Pain, fever, anti-thrombotic Box warning: CV, GI, bleeding risk, edema Indomethacin: potent anti-inflammatory activity *Ramsinghani--> non-compliance or discontinuation due to tinitis
Mobic Meloxicam *long acting (>6H) t1/2 life: 15-20 hours) Enolic Acid NSAID Derivative Reversible; non-selective COX inhibitor Inflammation, Pain, fever, anti-thrombotic Box warning: CV, GI, bleeding risk, edema Weak inhibition of proteoglycanase and collagenase *Heteroarylcarboxamide: longer plasma half-life (requires less frequent dosing) *no COOH group in your Oxicams) (*Some Cox-2 selectivity)
Feldene Piroxicam *long acting (>6H); t1/2 life: 38 hours) NSAID Reversible; non-selective COX inhibitor Inflammation, Pain, fever, anti-thrombotic Box warning: CV, GI, bleeding risk, edema Weak inhibition of proteoglycanase and collagenase *For oxicams (be able to point out an Enol structure (this is how Oxicams interact with the binding to Arg120 active site
Celebrex Celecoxib *long acting (>6H) NSAID Reversible; COX-2 selective inhibitor *Sulfonamide binds to Arg513 and Histidine; not Arg120 Inflammation, Pain, fever, Pro-thrombotic Box warning: SERIOUS CV and GI risks Why serious? blocking the COX-2--> more of the Arachidonic acid can be converted via COX-1 to form greater thromboxane (greater TxA2 activity) *Stilbene ring req'd for activity; sulfonamide group; only Coxib on market because of increaed risk of MI and Increased BP from Rofe/Valdecoxib *least COX-2 selective doesn't raise concerns for CV risk)
Voltaren, Pennsaid Diclofenac *short acting (<6H) Acetic Acid NSAID Derivative Reversible; non-selective COX inhibitor Inflammation, Pain, fever, anti-thrombotic Box warning: CV, GI, bleeding risk, edema Ramsing note: GSH cysteine residue containing SH group conjugates with ROS on quinoneimine metabolite forming detoxified GSH conjugate (non-toxic) Quinoneimine metabolite (ROS- reactive O2 species) -GSH (limited supply; body will use Hepatocytes (Liver toxicity via cysteine conj. with quin. metabolite. *Ext. met--> BA (50%) *LFT recommend
Relafen Nabumetone (Prodrug) *long acting (>6H) Propionic NSAID (Acetate Prodrug) Reversible; non-selective COX inhibitor Inflammation, Pain, fever, anti-thrombotic Box warning: CV, GI, bleeding risk, edema Non-acidic Prodrug *inactive and no acidic group -low gastric irritancy profile *Bypasses the Dual injury model *(no COOH/ activated in circulation) *active metabolite (6-Methoxynaphthylacetic acid)
Rheumatrex Methotrexate Non-biologic /Traditional DMARD Dihydrofolate reductase inhibitor -decreases purine production and DNA synthesis -Antifolate -increases adenosine Anti-inflammatory, anti-proliferative -extra-articular effect -infections and malignancy -Box warning (PO): Pregnancy (embryo-fetal toxicity; Hypersensitivty Folate Supplementation req'd *reduce incidence of MTX-related AE *DI: NSAIDS, Probenacid, and Penicillin G inhibti hOAT3 (decreasing MTX elimination) *MOA: inhibits B-cell proliferation; inhibits DHFR *anionic drug--> eliminated by OAT3) Active metabolites: 7-hydroxyMTX; MTX polyglutamate
Arava Leflunomide (PRODRUG) (t1/2 life: <1h) Non-biologic /Traditional DMARD Pyrimidine synthesis inhibitor Anti-inflammatory, anti-proliferative Infections and lymphomas; Box-warning: Pregnancy (embryonic lethality; teratogenicity) -Hepatotoxic PRODRUG, requires hepatic activation to its active metabolites -Requires drug clearance to pursue pregnancy *undergoes enterohepatic circulation extending DOA*** Removal can occur via Cholestyramine-mediated elimination *inhibits B-cell proliferation; inhibtion of DHODH (dihydroorotate dehydrogenase) rapidly met. to teriflunomide (t1/2 life: 15-18 days)
Plaquenil Hydroxychloroquine Non-biologic /Traditional DMARD Not all known -T-lymphocyte suppression -Decreaed leukocyte chemotaxis -Lysosome stabilization Reduce pro-immune factors -Malaria -mild SLE Ocular toxicity Cardiovascular events *unique (ability to bind to melanin--> accumulates in retinal cells and leads to degradation of the retina *Ha- Cardiac QTc-prolongation SLE treatment: Helps to control disease flares (decreases disease activity) -improves survival in pts -slow onset 1-6 months; used for long-term management *concentrates in the organs (t1/2 life: 40 days)
Azulfidine Sulfasalazine Non-biologic /Traditional DMARD Inhibits cytokine secretion -reduced ability to release IL-1/IL-6 Anti-inflammatory Sulfa or salicylate allergy contraindication; CI for GI or GU obstruction PRODRUG metabolites (5-ASA & sulfapyridine *Sulfapyridine--> metabolized by NAC to inactive acetylated metabolite POOR oral BA: bacterial enzyme break the nitrogen db into 2 portions: *5-ASA: anti-inflmmatory *Sulfapyridine: inhibit purine biosynthesis
Enbrel Etanercept Biologic/ TNF-a inhibitor Binds TNF-a; prevents binding to TNFR Moderate-severe RA; Reduce inflammatory response/ pain Box warning: Malignancy; TB risk TB test required
Remicade Infliximab Biologic/ TNF-a inhibitor Binds TNF-a; prevents binding to TNFR Moderate-severe RA; Reduce inflammatory response/ pain Box warning: Malignancy; TB risk TB test required
Humira Adalimumab Biologic/ TNF-a inhibitor Binds TNF-a; prevents binding to TNFR Moderate-severe RA; Reduce inflammatory response/ pain Box warning: Malignancy; TB risk TB test required
Cimzia Certolizumab Biologic/ TNF-a inhibitor Binds TNF-a; prevents binding to TNFR Moderate-severe RA; Reduce inflammatory response/ pain Box warning: Malignancy; TB risk TB test required
Actemra Tocilizumab Biologic Inhibits IL-6 Moderate-severe RA; Reduce inflammatory response/ pain Box Warning: Infection risk TB test required
Kevzara Sarilumab Biologic Inhibits IL-6 Moderate-severe RA; Reduce inflammatory response/ pain Box Warning: Infection risk TB test required
Simponi Golimumab Biologic/ TNF-a inhibitor Binds TNF-a; prevents binding to TNFR Moderate-severe RA; Reduce inflammatory response/ pain Box warning: Malignancy; TB risk TB test required
Kineret Anakinra Biologic Inhibits IL-1 Moderate-severe RA; Reduce inflammatory response/ pain infection, malignancy TB test required
Orencia Abatacept Biologic Inhibits T-cell activation -Blocks CD80/86 on APC Moderate-severe RA; Reduce inflammatory response/ pain infection, malignancy TB test required
Rituxan Rituximab Biologic Induces B-cell apoptosis -CD20 antibody Moderate-severe RA; Reduce inflammatory response/ pain Box warning: Infusion and mucocutaneous reactions TB test required
Xeljanz Tofacitinib DMARD Selective JAK inhibitor; decreases proliferation of NK, T & B cells Moderate-severe RA; Reduce inflammatory response/ pain Box waring: infection, malignancy, thrombosis TB test required
Olumiant Baricitinib DMARD Selective JAK inhibitor; decreases proliferation of NK, T & B cells Moderate-severe RA; Reduce inflammatory response/ pain Box warning: infection, malignancy, thrombosis TB test required
Rinvoq Upadacitinib DMARD Selective JAK inhibitor; decreases proliferation of NK, T & B cells Moderate-severe RA; Reduce inflammatory response/ pain Box warning: infection, malignancy, thrombosis TB test required
Imuran Azathioprine t1/2: 12 min 6-MP (3 hours) Immunosuppressant Ha: Converted to 6-MP (interferes with de novo purine synthesis producing faulty purines and inhib. DNA synthesis (decreased B cells and T-lymphocytes *Ha: appropriate for more severe symptoms and significant organ damage Ha: metabolism--> TPMT--> low enzyme activity can predispose to toxicity *Xanthine Oxidase *Pt may have TPMT deficiency *AE: Pancreatitis/ infertility/depresses spermatogenesis (less common) *Ha: Azathioprine: Steroid-Sparing *Ha: DI: allopurinol and febuxostat
Cytoxan Cyclophosphamide Immunosuppressant Ha: alkylates DNA, disturbing DNA synthesis and cell division; Metabolism--> Prodrug: requires CYP2B (liver) forming Acrolein (metabolite) *Ha: appropriate for more severe symptoms and significant organ damage Ha: Acrolein metabolite responsible for hemorrhagic cystitis (requires secondary drug : oral MESNA to prevent hemorrhagic cystitis Cyclophosphamide, Mycophenolate: usually in combo with steroids for severe lupus nephritis *Ha: give with steroid as combo (lower relapse rates, greater remission rates
Aspirin NSAID Irreversible binding -Non-selective COX inhibitor -COX-1 inhibition --> reduction in thromboxane inflammation, pain, fever, anti-thrombotic Box warning: CV, GI, bleeding risk, edema Reye's syndrome in children and young adults <20 yo, with viral fever
*Ramsinghani--> Clinorel Sulindac (Prodrug) Acetic Acid NSAID Derivative Bio-isostere of indomethacin -*Activated in circulation Less GI adverse effects than Indomethacin, Why? (See Other notes) Because the bio-activation of the drug occurs in the circulation. -Drug is not in the active form in the GI tract, so less side effects in GI
*Ha--> Cellcept, Myfortic Mycophenolate Immunosuppressant inhibits inosine monophosphate dehydrogenase (inhbiting B cell and T cell proliferation Alternative to cyclophosphamide for lupus nephritis GI, N/V/D, neutropenia, anemia, HTN, peripheral edema, infection, malignancy *Studies demonstrate similar efficacy and reduced toxiicty compared to Cytoxan
*Ha--> Benlysta Belimumab (2021) Immunosuppressant monoclonal antibody specific for soluble human B lymphocyte stimulator protein (BLyS) Indicated for pts with Active SLE while on standard therapy (*decreased disease activity and flare rates) *Active lupus nephritis: higher complete renal response infusion-related, injection-site rxn, hypersensitivity, infection, malignancy, depression Is it worth the cost?
*Ha--> Saphnelo Anifrolumab (2021) Immunosuppressant monoclonal antibody to the type 1 interferon (IFN) receptor for pts with moderate to severe SLE (but without severe active lupus nephritis or neuropsychiatric SLE infusion-related rxn, upper respiratory tract infections, herpes zoster, malignancy (skin cancer) Role is still being defined *modest benefit seen in disease activity, mostly pts with skin and joint disease *steroid sparing
Created by: Xander635
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