Who am I?

I am an Alkylating agent used to treat cancer

I form alkyl radicals that covalently bind with nucleophiles 

I produce intrastrand and interstrand DNA crosslinks blocking DNA and RNA replication and Apoptosis

Who am I?

I am a platinum complex drug used to treat cancer

I produce interstrand and intrastrand crosslinks in DNA inducing apoptosis

What is my MOA and what do I treat?

5-Fluorouracil

Antimetabolite

MOA: thymidylate synthase inhibitor (pyrimidine analog)

Used to treat cancer

Adverse effects: 

Mucositis from continuous infusion and bone marrow suppression from IV

Who am I?

I am a pyrimidine analog that inhibits DNA polymerase which inhibits DNA synthesis

What is my MOA and what do I treat?

Methotexate

Folic acid analog that inhibits dihydrofolate reductase

Inhibits DNA and RNA synthesis

Used to treat cancer

Adverse: bone marrow depression= secondary infections

Explain how I work and what drug I am combined with

Leucovorin rescue

Leucovorin= 5-formyl derivative of tetrahydrofolic acid used to replenish tetrahydrofolic acid levels

combined with methotrexate to treat cancer

Who am I?

I am a folic acid analog

I am used to treat cancer

I inhibit 3 enzymes (thymidylate synthase, dihydrofolate reductase, and glycinaminde ribonucelotide formyltransferase) which inhibits DNA and RNA synthesis

I am often combined with cisplatin as first line treatment

What is our common MOA and what do we treat?

Mercaptopurine and Thioguanine

Purine analogs that inhibit incorporation of purine derviatives into nucleic acids inhibiting DNA and RNA synthesis

Cancer Drugs

 Leukemia and lymphomas, IBS

Who am I?

I am an inhibitor of cancer cell-specific tyrosine kinase 

I inhibit tumor cell proliferation and stimulate apoptosis

I doubled the 5 year survival rate for chronic myelogenous leukemia from 31% to 59%

What is my MOA and what do I treat?

Bleomycin

DNA scission and fragmentation, inhibition of DNA repair mechanisms= inhibition of DNA synthesis 

SCC, testicular tumors and hodgkin's lymphoma

Do not use nitrous oxide sedation

Who am I?

I am a vinca alkaloid from the Madagascar periwinkle

I bind to tubulin and inhibit microtubule assembly arresting cell division in metaphase

I am used to treat Hodgkin's disease/lymphomas, bladder and testicular cancers

I am known to cause leukopenia and thrombocytopenia

Who am I?

I am a monoclonal anti-EGF receptor (Her2) = antagonist= induces cell cycle arrest

Used to treat breast cancer

What is my MOA and what do I treat?

Avastin (bevacizumab)

monoclonal anti-VEGF (blocking binding at VEGF receptor)

inhibits tumor-stimulated angiogensis

used to treat cancer

In what phase do I cause cell death?

Prednisone (as used for leukemia, lymphoma, multiple myeloma)

What is my MOA?

Tamoxifen

Selective estrogen receptor modulator= estrogen receptor antagonist

used to treat estrogen-dependent breast cancer, decrease risk of uterine cancer

Who am I?

I am an inhibitor of aromatase which inhibits estrogen synthesis

I am used to help treat breast cancer

What is our common effect?

Epogen and Procrit

Erythropoietin

Stimulation of red blood cells

used for anemia 

Who am I?

I am used to treat leukopenia

I stimulate the production of neutrophils 

Who am I?

I am an interleukin that stimulates the production of platelets

Who am I?

I am a keratinocyte growth factor used for severe oral mucositis

What is my MOA?

Zofran (ondansetron)

5HT3 receptor antagonist tha blocks central and peripheral vimiting reflex

Antiemetic

combining with apomoprhine can cause severe hypotension and loss of consciousness

What is our MOA and what do we treat?

Pepcid (famotidine), Tagamet (cimetidine), Zantac (ranitidine), Axid (nizatidine)

The "tidines"

Competitive H2 histamine receptor antagonist

inhibits histamine stimulated gastric acid secretion

used to treat PUD (peptic ulcer disease) and GERD (gastroesphogeal reflux disease)

What is our common MOA and what do we treat?

Prilosec (omeprazole), Nexium (esomeprazole), Prevacid (lansoprazole), Protonix (pantoprazole), Aciphex (rabeprazole)

The "prazoles"

Non-competetive covalent inhibitors of the proton pump H+K+ATPase

Used to treat PUD, GERD, erosive esophagitis

superior to the H2 antagonists (the tidines)

Who am I?

I react with sodium bicarbonate to form sodium alginate

gastric pH will cause this alginate to precipitate out

I am used to treat PUD and GERD

Who am I?

I am used to treat PUD and GERD

Aluminum hydroxide and sulfated sucrose form a gastroprotective viscous suspension that binds to ulcer sites

Who am I?

I am a prostaglandin analog used with NSAIDs to protective the GI system

What is my MOA and what do I treat?

Reglan (metoclopramide)

Dopamine receptor antagonist

relaxes pyloric and duodenal segments and increases peristalsis

used to treat delayed stomach empting due to diabetes or after surgery

also inhibits stimulation of the chemoreceptor trigger zone used as an antiemetic

What is our common MOA and what are we used for?

Compazine (Prochlorperazine) and Reglan (metoclopramide)

inhibits stimulation of the chemoreceptor trigger zone

used as antiemetics

Who am I?

I am a laxative

I am methycellulose which absorbs water and expands

This expansion causes increased pressure which stimulates excretion via water in stool

Metamucil

Who am I?

I am an anionic surfactant detergent used a laxative

Who am I?

I am a stimulant laxative that increases mucosal permeability allowing movement of fluid across the intestinal lumen

What is my MOA and what am I used as?

Linzess (linaclotide)

Stimulates intestinal guanylate cyclase which stimulates bowel muscle contractions

used as a laxative

What is my MOA and what am I used as?

Amitiza (lubiprostone)

Bonus: What drug should you not take with me?

activates ClC-2 chloride channels in intestinal membranes (fatty acid derived form of PGE1)

which increases intestinal fluid secretion and motility

used as a laxative

Bonus:

do not take zydelig (idelalisib) which is used to treat lymphocytic leukemia due to severe/fatal diarrhea

What are we and what do we treat?

Imodium (loperamide) and Lomotil (diphenoxylate)

opioid-like agents used to treat diarrhea

Lomotil is schedule V

Imodium alters motor function in the intestine delaying passage of fluid

Who am I and what do I treat?

Muscarainic receptor antagonist (antispasmodic)

Intestinal smooth muscle relaxant which reduces intestinal hypermotility

Bentyl (Dicyclomine)

used for IBS

Who am I?

I am an adsorbent and protectant used for diarrhea

Kaopectate (kaolin and pectin)

Kaolin is a natural hydrated aluminum silicate

What is my MOA and what do I treat?

Pepto Bismol (bismuth subsalicylate)

mechanism not well understood

coats intestinal tract

used for diarrhea/nausea/GERD, black tongue/black stool

What is our MOA and what do we treat?

Acyclovir and Valacyclovir

Guanosine analogs that selectively phosphorylate by viral thymidine kinase which inhibits viral DNA polymerase

Used to treat herpes

Valacyclovir is a prodrug of acyclovir that has better bioavailability

Who am I?

I am used to treat HSV infections that are resistant to acyclovir, CMV retinitis and pneumonitis 

I am a polymerase inhibitor

Cytovene (ganciclovir) IV only

Valganciclovir is a prodrug oral form of ganciclovir

What is my MOA and what do I treat?

Abreva (docosanol)

inhibits fusion between human cell membrane and HSV which prohibits entry into the human cell

used to treat herpes

Who I am?

I competitively inhibit neuraminidase on the surface of influenza virus particles

Used for influenza A and B

Do not used me for patients with asthma or COPD

Tamiflu (oseltamivir)

hydrolyzed to oseltamivir carboxylate in the liver

What is my MOA and what do I treat?

Selzentry (maraviroc)

CCR5 antagonist 

prevents CCR5 co-recptor (human) and gp120 subunut of virl envelope glycoprotein interaction via prevention of conformational change of gp120

Used to treat HIV/AIDS

What is my MOA and what do I treat?

Fuzeon (enfuvirtide)

Fusion inhibitor 

Gp41 initiates fusion of the virus into the lymphocyte cell surface

Prevents conformational changes and formation of entry pore

Used to treat HIV/AIDS

Who am I?

I am an inhibitor of reverse transcriptase 

I mimic naturally occuring nucleotides

I have significantly reduced the incidence of neonatal infection from 30% to 1%

I was the first NRTI (nucleoside reverse transcriptase inhibitor) developed for HIV/AIDS

Who am I?

I inhibit reverse transcriptase by binding to the enzyme adjacent to the active site

I am used to treat HIV/AIDS

I have a low resistance barrier

I can cause a false positive cannabinoid test

What is my MOA and what do I treat?

Invirase (saquinavir)

Inhibits HIV protease

this prevents proteins from being cut into usable pieces

leaves virons without the ability to infect other cells

used to treat HIV

Who am I?

I am a protease inhibitor used to treat HIV/AIDS

I am a strong inhibitor of CYP3A4

What is my MOA and what do I treat?

Isentress (raltegravir)

Integrase inhibitor used to treat HIV/AIDS

integrase creates available ends on viral DNA

What am I?

HAART

Highly Active Anti-Retroviral Therapy

combo drug of either a PI (protease inhibitor) or an NNRTI (non-nucleoside reverse transcriptase inhibitor) and two NRTIs (nucleoside reverse transcriptase inhibitor)

What is our common MOA and what do we treat?

Victrelis (boceprevir), incivek (telaprevir), Olysio (simeprevir)

the "previrs"

Protease inhibitors used to treat Hepatitis C

often combined with pegylated interferon and ribavirin for chronic hep C

What is my MOA and what do I treat?

Harvoni (ledipasvir and sofosbuvir)

Ledipasvir inhibits a key viral kinase

Sofosbuvir is a RNA polymerase inhibitor

Used to treat Hepatitis C

When combined with Ribavirin= 90% cure rate

Who am I?

I am the drug of choice for fungal infections of the oral cavity

I bind ergosterol and create pores in fungal cell membranes allowing K+ to leak out of the cell

I am used prophylactically for immunocompromised patients

I am only used topically

What is our common MOA and what do we treat?

Azoles 

Examples: Triazole and Imidazole

Inhibition of 14alpha-sterol demethylase

Fungal infections

Imidazole= simple candidasis

Triazoles for more extensive infections= metabolized slower and fever adverse effects/drug interactions

Who am I?

I am an antifungal that is well absorbed from the GI tract

I inhibit synthesis of testosterone and estradiol

Who am I?

I am an antifungal that is a triazole derivative 

I am a more selective inhibitor of fungal cell membrane 14alpha-sterol demethylase

Diflucan (fluconazole)

fluconazole resistant fungi are cross resistant to other azole antifungal agents

Who am I?

I am a triazole antifungal (same MOA)

I am used if infection is resistant to nystatin, ketoconazole, fluconazole, etc

I am also a significant inhibitor of CYP3A4

What is my MOA and what do I treat?

Diquinol (iodoquinol)

Halogenated hydroxyquinoline with amebicidal, antitrichomonal, antibacterial and antifungal activity

Chelates trace metals at bacterial surfaces that are essential for growth

used for angular cheilitis 

Who am I?

I am the most toxic antifungal

I have the same MOA as nystatin (binds to ergosterol and creates pore in fungal cell membranes allowing K+ to leak out)

What is our common MOA?

Echinocandins (The Fungins)

Cancidas (caspofungin), Eraxis (anidulafungin), Mycamine (micafungin)

Inhibit glucan synthase inhibiting synthesis of 1,3-beta-D-glucan which is essential for fungal cell walls

Specific for fungi since the target is not expressed in humans

Who am I?

I am converted to 5-FU then to 5-FdUMP and then 5-FUTP

5-FdUMP inhibits fungal thymidylate synthase which shuts down DNA synthesis

5-FUTP inhibits RNA synthesis

I am used for cryptococcal endocarditis and meningoencephalitis

Warning: I can cause myelosuppression

What is our MOA and when are we prescribed?

Noxafil (posaconazole) and Vfend (voriconazole)

Triazole antifungals: inhibition of 14alpha-sterol demethylase

prescribed when candida loses sensitivity to itraconazole