83 terms

HD4 Drugs

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Prednisone
Immunosuppressives
Glucocorticoids
Oral
Modulation of gene expression- decreased production of cytokines
Many indications.
Side effects: insomnia, weight gain, mood changes, cushing syndrome
Cyclosporin A
Immunosuppressives
Calcineurin inhibitor
oral and IV
calcineurin inhibitor- which leads to decrease IL-2 production and T-cell activation
Indications: prophylaxis organ rejection, chronic rejection, refractory RA and psoriasis
Side effects: Infx, nephrotox, HTN, Hyperlipidemia, diabetes
Tacrolimus
Immunosuppressives
Calcineurin inhibitor oral and IV
calcineurin inhibitor- which leads to decrease IL-2 production and T-cell activation
Indications: prophylaxis organ rejection in kidney, liver, heart transplants
Side effects: Infx, Nephrotoxicity, neurotox, hypercalcemia, secondary tumors, diabetes
Extensive cyp3a metabolism, fluconazole, ketoconazole (DDI's)
Sirolimus
Immunosuppressives
Anti-proliferative agents
Oral
Binds FKBP-12->inhibits mTOR->inhibits T-cell activation Indications: prophylaxis organ rejection-kidney
Side effects: Infx. peripheral edema, HTN, Hyperlipidemia
Azathioprine
Immunosuppressives
Anti-proliferative agents
oral and IV
prodrug- metabolized to 6-mercaptopurine. Inhibit DNA/RNA synthesis
Indications: prophylaxis organ rejection-kidney, Refractory active RA
Side effects: myelosuppression, mucositis
Cyclophosphamide
Immunosuppressives
Anti-proliferative agents
oral
bis-electrophile crosslinking agent
Indications: conditioning for BMT, RA
Side effects: ovarian failure, sterility, bladder toxicity, myelosuppression
Crosses BBB
Mycophenolate mofetil
Immunosuppressives
Anti-proliferative agents
oral and IV
Prodrug- inhibits IMP dehydrogenase-> de novo purine sythesis
Indications: prophylaxis Organ rejection
Side effects: Infx, diarrhea, leukopenia, teratogenic
Methotrexate
Immunosuppressives
Anti-proliferative agents
oral and IV
dihydrofolate reductase inhibitor-> DNA/RNA synthesis. polyglutamate forms inhibit thymidylate synthase
Indications: refractory RA and Psoriasis
Side effects: mucositis, infx, renal failure and infertility at high dose
ATGAM
Immunosuppressives
Biologicals
IV
Anti-thymocyte immunoglobulin->decreases circulating lymphos
Indications: management of allograft rejection-kidney
Side effects: Infx, thrombocytopenia, leukopenia, malignancies
Anti-CD-3 (OKT3)
Immunosuppressives
Biologicals
IV
Anti-CD3 Ab, reduce circulating T-cells, block antigen recognition strx
Indications: acute allograft rejection
Side effects: cytokine release syndrome, anaphylactic reaction, Infx
Cimetidine
GI drugs Tagamet OTC H2 receptor antagonist Reversible inhibitor of histamine binding to H2, inhibits stomach acid production Treatment of active duodenal ulcers and benign gastric ulcers, maintenance therapy of duodenal ulcer; GERD Well tolerated, diarrhea, headache, drowsiness, fatigue, constipation Increases level of drugs metabolized by CYPs Oral absorption, minimal liver metabolism, excreted in urine
Omeprazole
GI drugs
Prilosec OTC
H/K-ATPase inhibitor
Irreversible inhibitor of K+,H+ ATPase
Indications: Treatment of active duodenal ulcers and benign gastric ulcers, maintenance therapy of duodenal ulcer; GERD, H pylori
Side effects: Well tolerated, headache, dizziness, rash, GI effects
DDIs: May affect drugs metabolized by CYPs
Acid-mediated hydrolysis in stomach yields metabolite that reacts w proton pump. Uncharged drug is absorbed in intestine and doesn't really do much systemically. Metabolized by liver
Misoprostil
GI drugs
Prostaglandin
Anti-secretory and mucosal protective activity
Indications: Reduce risk of NSAID-induced gastric ulcers in patients at high risk of complications. Doesn't have effect with duodenal ulcers.
Side effects: Gi effects, CNS effects, Pregnancy category X, potential abortifacient
Esterified pro-drug rapidly activated, primarily excreted in urine. Needs 4x/day dosing.
Metoclopramide
GI drugs
Dopamine antagonist
Prokinetic agent, binds with endogenous dopamine for binding to receptor, also binds 5-HT receptors
Indications: PO- symptomatic treatment of diabetic gastroparesis, GERD; IV- prevalence or treatment of nausea and vomiting associated with chemotherapy.
Side effects: CNS effects, extra-pyramidal reactions, GI effects. *May cause irreversible tardive dyskinesia Oral, IV, IM, hepatic metabolism.
Loperamide
GI drugs
Immodium OTC
Opioid agonist
Anti-diarrheal, effects on intestinal motility, secretion, and absorption
Indications: Relief of acute nonspecific diarrhea and chronic diarrhea associated with IBD
Side effects: CNS effects (fatigue, dizziness, drowsiness), constipation
Pharmacokinetics: Oral, systemic absorption, doesn't cross BBB, hepatic CYP metabolism, excreted in feces
Sulfasalazine
GI drugs
Azulfidine 5-aminosalicylic acid
Unknown mechanism
Indications: Mild to moderate ulcerative colitis; prolongation of the remission period between acute attacks of ulcerative colitis
Side effects: CNS effects, GI, reversible oligospermia, allergic rxns, reduced folate absorption.
Oral administration of prodrug -> metabolized by colonic bacteria to 5-ASA (active)
Ondansetron
GI drugs
5-HT3 antagonist
Acts at central and peripheral receptors, blocks binding of serotonin that initiate vomiting reflex
Indications: Prevention of nausea and vomiting associated with cancer chemotherapy; radiotherapy; prevent of postoperative PONV (prevention of nausea vomiting), rare arrhythmias can occur!
Side effects: CNS effects, pruritis and rash, diarrhea, gynecological effects
Once a day dosing, tablet and IV formulations available, well absorbed following oral admin, extensive hepatic metabolism CYP and phase II, excreted urine and feces.
Dexamethasone
GI drugs
Corticosteroids
Anti-emetic
Side effects: Insomnia, mood changes, increased appetite, weight gain, Cushings, susceptibility to infection Pharmacokinetics: Oral, IV, topical, hepatic metabolism, excreted in urine and feces.
Aprepitant
GI drugs
Neurokinin1 receptor antagonist
Inhibits binding of substance P to the neurokinin 1 receptor Indications: Prevention of acute and delayed nausea and vomiting associated with chemotherapy, PONV
Side effects: use with caution in pts with severe hepatic impairment, CNS effects, diarrhea, constipation, nausea Drug interactions with antifungals and warfarin
Oral or IV administration, extensive hepatic metabolism
Scopolamine
GI drugs
Muscarinic receptor antagonist
Indications: PONV with motion sickness, recovery from anesthesia and surgery
Side effects: dry mouth, drowsiness
3 day dose, percutaneous absorption, patch must be placed behind the ear, metabolism, excretion not well characterized
Cyclophosphamide
Anti-neoplastics
Cytotoxic
DNA damage-alkylation-nitrogen mustards
Indications: Lots
Side effects: (many=myelosuppresion, mucositis, nausea, vomiting, alopecia, secondary malignancies- AML), causes BLADDER CANCER.
Crosses BBB
Busulfan
Anti-neoplastics
Cytotoxic
DNA damage-alkylation
Many indications.
Many side effects.
crosses BBB
Cisplatin
Anti-neoplastics
Cytotoxic
DNA damage-crosslinking Platinums
Indications: Testicular, ovarian, bladder metastatic cancers Side effects-Nephro, OTOTOXICITY, and secondary AML
Carmustine
Anti-neoplastics
Cytotoxic
DNA damage-alkylation-Nitrosoureas
Indications: Brain tumor, HL, NHL, MM
Side effects: Many-VOD-high dose, AML, myelodysplasia
Dacarbazine
Anti-neoplastics
Cytotoxic
DNA damage-alkylation-Triazines- methylating
Many indications.
Many Side effects-CNS tox. teratogenic, AML
Thiotepa
Anti-neoplastics
Cytotoxic
DNA damage-alkylation-crosslinking
Topotecan
Anti-neoplastics
Cytotoxic
DNA damage-Topoisomerase inhibitor-Topo I RELAPSED SMALL CELL lung cancer
Many side effects.
Etoposide
Anti-neoplastics
Cytotoxic
DNA damage-Topoisomerase inhibitor-Topo II
Indications: refractory testicular and small cell lung
Side effects: many
Doxorubicin
Anti-neoplastics
adriamycin
Cytotoxic
DNA damage-Topoisomerase inhibitor-Topo II
Many indications.
Side effects: numerous, CARDIOTOXICITY.
Bleomycin
Anti-neoplastics
Cytotoxic
DNA damage- free radicals
Many indications.
Side effects: numerous, PULMONARY TOXICITY.
Dactinomycin
Anti-neoplastics
Cytotoxic
DNA damage- free radicals
Indications: childhood tumors=Wilms, Rhabdomycosarcoma, germ cell, Ewings.
Numerous side effects.
Methotrexate
Anti-neoplastics
Cytotoxic
Antimetabolites-Folic acid analogs
Leucovorin
Anti-neoplastics
Cytotoxic
Antimetabolites-Folic acid analogs- participation in one carbon transfer
Methotrexate OD RESCUE MEDICATION, use with 5-FU to enhance toxicity
Fluorouracil
Anti-neoplastics
Cytotoxic
Antimetabolites-Pyrimidine analog-inhibits thymidylate synthase-> DNA synthesis Lots- skin malignancies many
Gemcitabine
Anti-neoplastics
Cytotoxic
Antimetabolites-Pyrimidine analog
Indications: pancreatic, non-small cell lung, breast and ovarian.
Side effects: many- pulmonary tox, infusion rxn
Mercaptopurine
Anti-neoplastics
Cytotoxic
Antimetabolites-Purine analog, inhibits PRPP
Indication: ALL
Many Side effects- teratogenic, carcinogenic
Pentostatin
Anti-neoplastics
Cytotoxic
Antimetabolites-Purine analog
Indication: Hairy Cell Leukemia
Many side effects
Paclitaxel
Anti-neoplastics
Cytotoxic
Antimetabolites-Mitotic poisons- inhibits MT polymerization
Indications: many, incl. kaposi sarcoma
Side effects numerous, incl. neurotox.- peripheral neuropathy
Vinblastine
Anti-neoplastics
Cytotoxic
Antimetabolites-Mitotic poisons- inhibits MT polymerization
Many applications
Many side effects, incl neurotox
L-asparaginase
Anti-neoplastics
Cytotoxic
Antimetabolites- decreases levels of asparagine-> inhibits protein synthesis
Indication: ALL
Side effects: Many-bleeding problems
Hydroxyurea
Anti-neoplastics
Cytotoxic
Antimetabolites-inhibits Ribonucleotide reductase-denovo DNA synthesis
Indications: melanoma, CML, refractory ovarian
Side effects: Many- maculopapular rash
Mitotane
Anti-neoplastics
Non-cytotoxic
Hormone and antagonist-adrenocortical
Indications: adrenocortical cancer
Side effects: adrenal insufficiency
Tamoxifen
Anti-neoplastics
Non-cytotoxic
Hormone and antagonist-Selective estrogen receptor modulator
Indications: Breast cancer
Side effects: Estrogen related symptoms- menopausal, VTE, endometrial hyperplasia
Anastrozole
Anti-neoplastics
Non-cytotoxic
Hormone and antagonist-Aromatase inhibitor
Indications: Breast cancer with Estrogen receptor positivity/overexpression
Side effects: asthenia, arthralgia, peripheral edema
Flutamide
Anti-neoplastics
Non-cytotoxic
Hormone and antagonist-Antiandrogen
Indications: Prostate cancer
Side effects: Hot flashes, decreased libido, gynecomastia
Tretinoin
Anti-neoplastics
Non-cytotoxic
Hormone and antagonist-Retinoid differentiating agent
Indication: AML
Side effect: Vit. A toxicity, retinoic acid syndrome(fever, leukocytosis, dyspnea, wieght gain, pulm. infiltrates, pleural effusions), cardiac problems
Imatinib
Anti-neoplastics
Non-cytotoxic
Targeted therapeutics-Protein tyrosine inhibitors, binds and leads to growth arrest
Indications: CML, myelodysplastic syndrome, ALL w/ philidelphia chromosome, GI stromal tumors
Gefitinib
Anti-neoplastics
Non-cytotoxic
Targeted therapeutics-Protein tyrosine inhibitors
Indications: Non small cell lung refractory to platinum therapy.
Side effects: HTN, elevated liver enzymes, dry skin.
Cetuximab
Anti-neoplastics
Non-cytotoxic
Targeted therapeutics-Monoclonal antibodies- anti EGFR
Indications: EGFR expressing colorectal cancer
Side effects: asthenia, malaise, infusion related Sx's
Trastuzamab
Anti-neoplastics
Non-cytotoxic
Targeted therapeutics-Monoclonal antibodies- anti HER2
Indications: Node positive HER-2 overexpressing breast cancer and gastric cancer
Side effects: infusion related Sx's, cardiotoxicity
Bevacizumab
Anti-neoplastics
Non-cytotoxic
Targeted therapeutics-Monoclonal antibodies- Anti VEGF
Indications: Many- NOT breast
Side effects: wound healing complications, GI perforations, VTE,
Bortezomib
Anti-neoplastics
Non-cytotoxic
Targeted therapeutics- proteosome inhibitor-> down reg. of NFkB
Indications: Multiple Myeloma
Side effects: Many- orthostatic hypotension
Oseltamivir
Anti-viral prodrug
Inhibit viral particle release
influenza A and B
Indications: acute therapy less than 2 days Sx's, and prophylaxis.
Side effects: Rare- steven johnson syndrome, anaphylaxis Renal elimination
Foscarnet
Anti-viral
DNA pol inhibitor
Indications: Inhibits DNA polymerase CMV, HSV,VZV
Acyclovir
Anti-viral
DNA pol inhibitor
Prodrug- activated by thymidine kinase-> inhibits viral DNA polymerase
Indications: Prim. and Sec. HSV VZV, prophylaxis in BMT.
Side effects: very few
Ganciclovir
Anti-viral
DNA pol inhibitor
Prodrug- activated by CMV and inhibits DNA polymerase.
Indications: immuno compromised->CMV retinitis, pneumonia, GI lesion
Side effects: Cytopenias
AZT/zidovudine
Anti-viral
NRTI
Prodrug-Nucleoside analog reverse transcriptase inhibitors (NRTI)- inhibits RT and inserts into viral genome inhibiting elongation
Indications: HIV infx, PEP, reduce vertical transmission, also for HBV
Side effects: BM suppresion, anemia, lots of others. not well tolerated
Nevirapine
Anti-viral
NNRTI
Non-nucleoside analog reverse transcriptase inhibitors (NNRTI)- only inhibits RT but at a different site than NRTI
Indications: Combination therapy for HIV-1, reduce vertical transm.
Side effects: Skin reactions, Induce CYP 450
Ritonavir
Anti-viral
Protease Inhibitor (PI)
HIV protease inhibitor- inhibits maturation of HIV polyprotein
Indications: combination therapy
Indinavir
Anti-viral
Protease Inhibitor (PI)
HIV protease inhibitor- inhibits maturation of HIV polyprotein
Indication: comination therapy
Enfuviritide
Anti-viral
HIV infusion inhibitor
sub Q administration 2X daily
HIV fusion inhibitor- small peptide binds to gp41.
Indications: HIV-1 infection that is still replicating despite other retroviral therapy
Side effects: injection site rx, pneumonia, hypersensitivity
Raltegravir
Anti-viral
HIV integrase inhibitor
HIV integrase inhibitor same as enfuviritide
Side effects: myopathy and rhabdomyolysis
Maraviroc
Anti-viral
CCR5 receptor antag.
CCR5 co-receptor antagonist
Indications: HIV-1 that is CCR5-tropic
Side effects: Hepatoxicity-preceded by rash and systemic allergic rxn.
Chloroquine
Anti-parasitic
antimalarial
oral
Mechanism poorly understood
Treatment of acute malarias (all)
Side effects: Ocular and Ototoxic at high dose
Mefloquine
Anti-parasitic
antimalarial
oral
Mechanism poorly understood
Indications: Mefloquine susceptable falciparum and vivax
Side effects: CNS- nightmares, seizures, hallucinations ketoconazole and halofantrine
Primaquine
Anti-parasitic
antimalarial
oral
Indications: destroys latent hepatic and tissue forms radical cure- not for erythrocytic stages
Side effects: Hemolytic anemia w/ G6PD def.
Quinine
Anti-parasitic
antimalarial
oral
kills erythrocytic forms uncomplicated falciparum cases when other better drugs are not available.
Side effects: tinnitus, visual effects, hypoglycemia, hemolytic anemia with G6PD def
Malarone
Anti-parasitic
antimalarial
oral
inhibit pyrimidine biosynthesis
Indications: Prophylaxis, acute uncomplicated P. falciparum
Side effects: headache, GI
Artemether/lumafantrine (coartem)
Anti-parasitic
antimalarial
oral
Mechanism not known
Indications: Acute uncomplicated falciparum
Side effects: hypersensivity- uticaria & angiodema
Metronidazole
Anti-parasitic
antiamebal/systemic topical, oral, IV
prodrug- damages DNA
Indications: Trichomoniasis, amebiasis, anaerobic infx
Side effects: avoid ALCOHOL, CNS-ataxia, vertigo, dizziness
Nitazoxanide
Anti-parasitic
oral
interferes with energy production
Indications: giardia, cryptosporidium
Side effects: GI and headache
Paromomycin
Anti-parasitic
luminal anti amebal
interferes with protein synthesis
Indications: intestinal amebiasis (not extraintestinal)
Side effects: GI-nausea, diarrhea
Mebendazole
Anti-parasitic
antihelminthic
oral
binds to worm tubulin. interferes with organelle transport Indications: enterobiasus, trichuris, ascariasis, ancylostoma
Few side effects
Praziquantel
Anti-parasitic
antihelminthic
oral
increased calcium permeability
Indications: wide use shistosoma, chlonorchis
Side effects: GI, rash, DO NOT GIVE WITH RIFAMPIN
Nystatin
Anti-fungal
topical only
same as amphotericin B
Superficial infection- topical
Griseofulvin
Anti-fungal
Oral
inhibits mitotic function- high affinity for keratin
Indications: Superficial infection/oral admin- epidermophyton, microsporin, trychophyton (NOT candida)
Side effects: GI, headache p-450 inducer
Clotrimazole
Anti-fungal
topical only
similar to ketoconazole
Indications: Superficial infection/TOPICAL
Terbinafine
Anti-fungal
oral, Topical.
Inhibits fungal ergosterol synthesis: squalene epoxidase inhibitor (accumulates hair, nails, skin)
Indications: Superficial infection: skin trychophyton and candida
Side effects: GI and liver problems
Amphotericin B
Anti-fungal
Parenteral, oral, IV
forms pores in cell. has high affinity for ergosterol (fungal version of cholesterol)
Indications: disseminated systemic infx, oral-bowel candida infx
Lipid formulations-decrease side effects, nephrotoxicity, anemia, thrombopenia, leukopenia, poor oral absorption. No CNS distribution-have to give intrathecally
Flucytosine (5-fluorocytosine)
Anti-fungal
Oral
Prodrug-(specifically activated in fungi)
5-FU interferes with DNA (Thymidylate sythase)/RNA sythesis
Indications: Systemic infection
Side effects: Rigors, aches, GI, leukopenia, thrombopenia, Don't use with renal impairment
DDI with Amphotericin B- can cause renal impairment- but often used together distributes to CNS
Ketoconazole
Anti-fungal
oral
inhibits fungal ergosterol synthesis
Indications: Systemic infection
Side effects: effects of human sterol synthesis inhibition-hepatic toxicity, gynocomastia CYP450 interactions. Doesn't cross BBB
Fluconazole
Anti-fungal
antifungal/triazole
oral
inhibits fungal ergosterol synthesis
Indications: Systemic infection. oropharyngeal and esophageal candidiasis
Side effects: Less toxic than ketoconazole but similar profile. Hepatoxicity, GI, thrombocytopenia, reversable alopecia CYP450 interactions DOES cross BBB
Caspofungin
Anti-fungal
IV only
inhibit fungal cell WALL synthesis
Indications: Systemic infection/IV only: invasive aspergillus and candida