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General pharmacology
| Question | Answer |
|---|---|
| Cyclophosphamide | Alkylating agent prodrug converted to nitrogen mustard and acrolein by CYP2B6 in liver. Tx-> CLL, solid tumors, NHL, ovarian carcinomas, neuroblastoma, and immunosuppression in SLE.AE->chemical cystitis(acrolein), SIADH, myelosupression, amenorrhea/azoosp |
| List the drugs used for standard breast cancer combination chemotherapy. | Cyclophosphamide, methotrexate, 5-fluorouracil (paciltaxel may also be used over the second time if metastisis occurs). |
| List the drugs used for standard colorectal cancer | 5-fluorouracil, oxaliplatin, leukovorin |
| List the drugs used for standard ovarian cancer combination therapy. | Cisplatin and pacilitaxel |
| List the combination of chemotherapy used for testicular cancer. | Cisplatin, bleomycin, vinblastin |
| Non-hodgkin lymphoma combination chemotherapy. | cyclophosphamide, doxorubicin, vincristine, prednisone |
| Hodgkins Disease combination chemotherapy. | Mechlorethamine, vincristine, procarbazine, prednisone. or doxorubicin, bleomycin, dacarbazine, vinblastin |
| chemotherapy agents showing decreased effectiveness with changes to sensitivity of target enzyme. | Fluorouracil (thymidylate synthetase), mercaptopril (purine interconversion enzymes), methotrexate (dihydrofolate reductase) |
| chemotherapy agents showing decreased effectiveness with changes to target receptor characteristics. | methotrexate receptor |
| chemotherapy agents showing decreased effectiveness through increased functioning of P glycoprotein transport (mdr gene) | dactinomycin, doxorubican, paclitaxel, vincristine, vinblastine, etoposide. |
| chemotherapy agents showing decreased effectiveness with modifications to drug-inavtivating enzymes | cytarabine and mercaptopurine |
| chemotherapy agents showing decreased effectiveness with increased DNA repair mechanisms in cancer cell. | cisplatin, cyclophosphamide, procarzapine, and other alkylating agents. |
| chemotherapy agents showing decreased effectiveness with reduced activation of drugs. | All prodrugs, cytarabine, doxorubicin, fluorouracil, mercaptopurine, methotrexate, thioguanine. |
| Chemotherapy agents with pronounced renal toxicity. | cisplatin (No BMS) and methotrexate. |
| Chemotherapy agents with pronounced Hepatic toxicity | 6-mecrapurine, cyclophosphamide, busulfan. |
| Chemotherapy agents with pronounced pulmonary toxicity. | Bleomycine (no BMS), busulfan, procarbazine. |
| Chemotherapy agents with pronounced cardiac toxicity. | Doxorubicin and daunorubican |
| Chemotherapy agents with pronounced neurologic toxicity. | Vincristine (no BMS) and cysplatin |
| Chemotherapy agents with pronounced immunosuppression effects. | cyclophosphamide and methotrexate |
| Chemotherapy agents with pronounced hemorrhagic cystitis and hematuria toxicity | cyclophosphamide |
| Chemotherapy agents with pronounced leukemia toxicity | procarbazine |
| Chemotherapy agents with pronounced pancreatitis toxicity. | asparaginase. |
| methotrexate | Tx solid tumors such as choriocarcinoma, osteogenic sarcoma, ALL. MOA through inhibition of dihydrofolate reductase therefore preventing THF from being made. Antidote- leukovorin (folinic acid). SE with nephrotoxicity, GI mucositis/diarrhea/GI ulceration |
| 5-fluorouracil (floxuridine) | Tx metastatic breast cancer, GI/ovary/bladder/prostate/pancrease/oropharyngeal cancers, hepatoma. MOA prodrug thymidylate synthase inhibitor. SE anorexia/alopecia/stomatitis/myelosuppression |
| Cytarabine | Tx AML. MOA pyrimidine analog blocking elongation of DNA strand. SE neurotoxicity |
| Azathioprine and mercaptopurine | Tx cancer chemotherapy, immunosuppressives, disease modifying antirheumatic drugs.MOA PRPP synthetase. SE BMS, leucopenia, thrombocytopenia, hepatotoxic-cholestasis. |
| Cyclophosphamide | alkylating agent produg; active metabolite nitrogen mustard forming carbonium ion intermediates; acrolein causing hemorrhagic cystitis (mesna);need high water load;nephrotoxic/myelosuppression/amenorrhea/azoospermia/leukemogenic/SIADH(demeclocycline) |
| Doxorubicin | binds topoisomerase 11 preventing helical break repair and causes ROS formation; only given IV with SM leading to extravasation (dimethyl sulfoxide); serious cardiomyopathy (dexrazoxane) |
| Dactinomycin | Binds DNA preventing DNA dependent RNA synthesis and causes breaks with ROS; Tx-rhabdomyosarcoma/wilms tumor/ewings tumor/kaposis sarcoma; SE-hematopoietic suppression/pancytopenia/proctitis/glossitis/cheilitis/alopecia |
| Bleomycin | mixture of 2 copper chelating peptides that fragments DNA in G2 phase; used as adjuvant with testicular canceres, squamous carcinomas of the head/neck/lungs, lymphomas; pulmonary toxicity/fibrosis, hyperthermia (especially w/ lymphomas), hyperkeratosis |
| cytarabine | antimetabolite pyramidine analog; blocks DNA stand elongation; used for AML; causes neurotoxicity |
| vincristine | antimitotic spindle poison that binds tubulin to prevent assembly of microtubules blocking the M phase; Tx- hematological malignancies, breast/germ cell/lung cancers, Hodgkins diseases (MOPP), rhabdomyosarcoma, neuroblastomas*; Very neurotoxic |
| Vinblastin | antimitotic spindle poison that binds tubulin to prevent assembly of microtubules blocking M phase; Tx testicular carcinoma (VBC/VBE); reversibly myelosuppressive/dose-limiting neutropenia/leucopenia/alopecia |
| Etoposide | stabalize Topoisomerase II/DNA complex causing double-strand DNA breaks during S and early G2 phases; Tx- VBE for testicular carcinoma/diffuse lymphomas/hodgkins diease/oat cell carcinoma of lung; SE-dose-limiting leukopenia*/may lead to AML*/skeletal |
| Topotecan | topoisomerase 1 inhibitor preventing re-ligation of bits of helices causing single stranded breaks in DNA; Tx- Colorectal/ovarian/small cell carcinomas; SE-neutropenia*(dose-limiting)/mucositis |
| Paclitaxel | taxanes inhibit microtubule disassembly, cuasing abnormal and dysfunctional spindles by binding to beta tubulin units; Tx-Advanced ovarian cancer*(CCCP)/metastatic breast carcinoma/metastatic non-small cell lung cancer (docetaxel); SE- hypersensitivity |
| Tamoxifen | prodrug metabolized by CYP2d6 to active endoxifen blocks binding of estrogen to estrogen receptors in estrogen-receptor positive breast carcinoma; Tx- breast cancer treatment and prophylaxis; CI-SSRI/paroxetine/fluoxetine; SE-menorrhea/menopause like/^Ca |
| Cisplatin | Platinum analog liipophilic prodrug hydrolyzed to active compound that reacts with DNA leading to breaks and miscoding(amifostine); interaction with cell cycle phase is cell specific;IV; need hydration with dose; nephrotoxic/ototoxic/nausea(ondansetron) |
| Carmustine | alkylating agent toxic to CNS used for CNS cancers. |
| Daunorubicin | Used to treat leukemia |
| topotecan | unique topoisomerase I inhibitor that prevents re-ligating of exposed bits of helices leading to accumulation of single-strand breaks in DNA. Dose-limiting and may cause neutropenia. |
| Fulvestrant | Antiestrogen for hormone-sensitive tumors. |
| Anastroozole | aromatase inhibitor used to prevent estrogen formation in in estrogen-sensitive tumors, mostly breast. |
| Leuprolide | GnRH agonist- when blood levels are constant, LH and FSH release are inhbitited. used to treat prostate cancer. |
| Prednisone | commonly used as adjuvant in chemotherapy combinations. |
| Rituximab | unconjugated chimeric anti-CD20 antibody that binds to CD20 of B-cells in Non-hodgkin lymphoma. |
| hydroxyurea | inhibits ribonucleotide reductase which stops the conversion of ribonucleotides to DNA which is used to tx myeloproliferative disorders |
| Imatinib mesylate | inhibits BCL-ABL in CML |
| Trastuzumab | monoclonal antibody against Her2/neu receptor tyrosine kinase which prolongs the survival of Her2/neu receptor positive metastatic breast cancer when combined with cytotoxic therapy |
| Phase S acting chemotherapy agents | methotrexate(dihydrofolate reductase) 5-fluorouracil(thymidylate synthase) Cytarabine(DNApolymerase) Floxudine(thymidylate synthase) mercaptopurine(purine nucleotide interconversion) hydroxyurea(ribonucleotide reductase) |
| Phase G2 acting chemotherapy agents | Bleomycin (fragments DNA) |
| Phase M acting chemotherapy agents | Vincristine/vinblastin(- microtubule polymerization) paclitaxel(- mictotubule depolymerization) |
| Phase G1 acting chemotherapy agents | Dactinomycin(binds DNA (-) DNA dependent RNA synthesis)tamoxifen (antiestrogen) |
| Between S and G1 phase acting chemotherapy agents. | Etoposide(interferes with topoisomerase II) Dactinomycin (binds DNA preventing DNA-dependent RNA synthesis) |
| Chemotherapy agents with irreversible toxicity towards particular organs giving them a cumulative toxicity. | Methotrexate, cisplatin, doxorubicin, bleomycin, vincristine |
| Busulfan | alkylating agent; CML selective depression of granulocytopoesis, AML, BM transplant prophylaxis; pulmonary fibrosis, hyperpigmentation |
| Asparaginase | Converts L-asparaginase to aspartic acid/ammonia; Tx-ALL* (very common adjuvant); given IV; SE-hypersensitivity/neurotoxic (coma)/hepatotoxic (delayed;bleeding/clotting risk) |
| Acute gouty arthritis pain control. | Ibprofen, indomethacin=NSAIDs; prednisone=glucocorticoids; colchicine=microtubule assembly inhibitor |
| Long term chronic gout management | probenecid & sulphinpyrazone=uricosurics; Allopurinol & febuxostat=xanthine oxidase inhibitors; Rasburicase, pegloticase=recombinant uricases |
| Causes of increased uric acid production | high purine intake (red meat), cancer treated w/ antineoplastics (methotrexate), inherited diseases (gout; lesch-Nyhann disease). |
| Causes of decreased uric acid excretion | alcohol consumption (especially fermented brews), obesity and triglyceridemia, pathology of the nephron resulting in poor filtering and poor secretion of uric acid. |
| MOA of gout caused by alcohol consumption | microbial fermentation produces purines, Higher NADH:NAD+ ratio favors high lactate:pyruvate ration and lactic acid out-competes uric acid at acid transporter site in nephron. |
| Probenecid | inhibits urate reabsorption in the lumen of the nephron in proximal tubule to increase uric acid secretion (opposite of penicillin which inhibits secretion). given orally. may prevent excretion of PEDs into urine and is part of DSP. |
| Sulphinpyrazone | inhibits uric acid reabsorbtion in the proximal convoluted tubule. subtherapeutic doses inhibit uric acid secretion. |
| Allopurinol | long term tx of hyperuricemia by inhibiting xanthine oxidase as active metabolite alloxanthine= non-competitive inhibitor; probenecid t1/2 higher and alloxanthine cleared faster; decrease breakdown of azathiaprine/mercaptopurine; increases theophylline |
| Colchicine | antimitotic antiinflammatory specific for acute gout pain by (-) microtubule formation= decreased WBC migration, LPO enzymes, synthesis of inflammatory leukotrienes (LTB4).excreted by MDR protein pump ((-) verapmil=increase). SE-GIT toxicity, low ADH |
| Drugs against circulating proinflammatory cytokines | infliximab, adalimumab, etanercept, anakinra |
| cytotoxic drugs used in RA treatment | methotrexate, azathioprine, leflunomide, cyclosporine |
| Infliximab | human/mice IgG1 monoclonal Ab against TNF-a. given IV with oral methotrexate (4 RA). Tx crohns disease, ulcerative colitis, RA, ankylosing spondylitis, psoriatic arthritis, IBD. SE-hypersensitivity Rx, infections, lymphoma(azothioprine), HF, AP |
| Adalimumab | humanized IgG1 Ab against TNF-a and decrease CRP, MMP-1/MMP-3, IL-6, ESR. Tx- RA, ankylosing spondylitis, crohns disease, psoriasis w/ arthropathy. given SC. SE-Black box infections, exacerbates CHF, serious infections, lupus-like syndrome. |
| Etanercept | human IgG1 Ab and receptor that binds TNF-a. Tx RA, psoriatic arthritis, juvenile arthritis by fusing TNF-a & TNF-B to receptor. SE- IV site Rx, autoantibody formation, hypersensitivity Rx, infections, increased cancer risk. CI-MS, live vaccine |
| Anakinra | Human IL-1 receptor antagonist. short t1/2. Tx- RA. SE-strong IV site Rx, decrease WBC, autoantibody. |
| Penicillamine | Given when other drugs fail to Tx RA. unknown MOA, but chelates Cu++ in wilsons disease (primary Tx). Given orally. SE-skin lesions, BMS, autoimmune syndrome, taste disturbance, hypersensitivity. CI-goodpasteures syndrome, MS, pregnancy |
| hydroxychloroquine/chloriquine | second line Tx of RA, but first line antimalarial; also SLE tx. MOA- T cell suppression, (-)WBC chemotaxis, stabalize lysosomal membranes, (-)DNA/RNA synthesis, traps ROSs. Given Orally w/o effect for 4-12 wks. SE-irreversible retinal degeneration |
| Sulfasalazine | Prodrug antiinflammatory COX inhbitor in the gut. Tx-ulcerative colitis, IBD, RA. SE-leukopenia, thrombocytopenia, alopecia, stomatitis, elevated liver enzymes, N/V/D GI Rxs |
| Azathioprine | MOA-prodrug that converts to 6-thioguanine in order to inhibti dihydrofolate reductase to (-) DNA/RNA synthesis. Adjunct for kidney transplants, and RA. SE-BMS, hepatotoxic, myalgia, infection, fever, malaise. |
| Leflunomide | inhibtis dihydroorotate dehydrogenase to (-) de novo pyrimidine synthsis. Tx- RA and psoriatic arthritis. AE-GI toxic, hepatotoxic, hersensitivity Rx, teratogenic, renal impairment, cytopenias. |
| Cyclosporine | inhibits calcineurin to (-) IL-2/IL-2R production-> decreasing activation of CD4 cells. Tx-transplant rejection prophylaxis, RA, psoriasis, nephrotic syndrome, BM rejection. SE-nephrotoxic, hypertension, high triglycerides, hypertension, hershutism |
| Malarone | Proguanil+atovaquone. MOA-plasmodial dihydrofolate reductase inhibitor. Use-prophylaxis of chloroquine-resistant and multi-drug resistant strains of P falciparum and P vivax. |
| Primaquine | drug of choice for P vivax and P ovale and prophylaxis for all malarial species with exo-erythrocidal, cametocytocidal, and hypnozoitocidal effects. |
| Chloroquine | 1st line tx for P vivax, P ovale, and uncomplicated falciparum malaria concentrating acid environment in vacoules of susceptible plasmodia iniside RBCs.inhibits polymerisation of heme, and actions of TNF-a. |
| Non-depolarizing blockers acting at the end plate of skeletal muscle. | pancuronium, vercuronium, atracurium, cisatracurium, mivacurium, rocuronium. |
| depolarizing blockers acting at the end plate of skeletal muscle | Succinyl chlorine |
| Spasmolytic CNS synapse of spinal cord and cortex acting muscle relaxants. | diazepam/lorazepam, baclofen, tizanidine, gabapentin |
| Properties of non-depolarising relaxants | Given IV to promote flaccid paralysis. eys>face>feet>hands>limbs>neck>trunk> intercostals>diaphragm for funtion, opposite for recovery. |
| Succinyl Choline | Given IV w/ fastest onset and shortest duration. SE- fasciculations->myalgia, hyperkalemia, arrhythmias, myoglobinemia, and malignant hyperthemia. |
| Motor endplate blocking drugs | can be specific for onset time, duration, recovery time, and side effects. highly polar quarternary positively charged ammonium limits lipid solubility and crossing of BBB. |
| List of muscle relaxants in order of duration of action | Tobocurarine (1)>Pancuronium (6XT)> Rocuronium (low)> vecuronium (6XT)>Atracurium (plasma esterases/laudanosine/1.5XT) >mivacurium (o.8XT)> succinylcholine (suxamethonium) |
| List of drugs that potentiate NMJ blockade. | quinidine, furosemide, lidocaine, amphotericin B, aminoglycosides, tetracyclines, Ca2+ channel blockers, general anesthetics, dantrolene. |
| List of drugs that antagonize non-depolarizing blockers | Phenytoin and carbamazepine (pancuronium and vecuronium), steroids, theophylline. |
| Baclofenal (lioresal) | GABA derivative agonist of presynaptic GABAbR in spinal cord & brain. given orally or intrathecally. Tx-MS, neuropathic pain, trigeminal neuralgia, spacticity (intrathecally), ALS. AE- hallucinations, CNS depression, paradoxical spasticity. CI-abrupt w/d |
| Diazepam/Lorazepam | Benzodiasepines that amplify GABAergic transmission in the cord, cerebrum, and cerebellum by binding the GABAR to increase the affinity of GABA/GABAR. Tx-anxiolytics, sedatives, myorelaxants, antiseizure; MS, stiff mans syndrome, and spasms. |
| Tizanidine | Cogener of Clonidine, a-2 agonist of pre- and post-synaptic adrenoceptors. Tx-spasticity associated w/ cerebral and spinal disease such as MS and ALS. AE- somnolence. |
| GABApentin | acts on a-2 delta subunit of presynaptic voltage-gated Ca2+ channels. amino-acid analogue of GABA. Tx-generalized tonic-clonic seizures, partial seizures, and spasmolytic.SE- somnolence & ataxia. Crosses BBB. |
| Dantrolene | acts w/in skeletal muscle to block Ca2+ from SR stores by interfering w/ ryanodine receptors. Tx- malignant hyperthermia antidote, cerebral palsy in hemi-/paraplegic pts, neuoroleptic malignant syndrome, serotonin syndrome. SE-weakness, hepatotoxic |
| Botulinum toxin | protein enzyme produced by clostridium botulinum. MOA-endocytosed by peripheral cholinergic nerve terminals, cleaves synaptobrevin preventing fusion of vesicles (-) AcH release. Given IM. Tx-muscle relaxant. SE-hypersensitivity,adverse spread |
| Malignant hyperthermia | AD disorder of skeletal muscle that contains abnormal ryanodine receptors-> uncontrollable IC Ca2+ releasse from SR when given succinyl choline, fluorodinated inhaled anesthetics. CP-hyperthermia, metabolic acidosis, tachycardia, contractures |
| Levamisole | Stimulates the maturation and proliferation of T cells. adjuvant for Dukes stage C colon cancer after surgical resection w/ 5-flourouracil/leucovorin. SE-Agranulocytosis |
| Bacillus-Calmette Guerin (BCG) | attenuated live mycobacterium bovis non-specific immunostimulant to promote T-cell mediated antitumor effects. Tx-intravesicular bladder cancer. SE-chemical cystitis. |
| Thalidomide | inhibitor of TNF-a production and used to Tx-erythema nodusum leprosum and cronhs disease. SE-teratogenic. |
| Interferon alpha | Class I recombinant cytokine used to increase the expression of MHC I and decrease expression of MHC II. Tx-HBV, HCV, HPV, malignant melanoma, CML, hairy cell leukemia, AIDs related Kaposi Sarcoma, Bahcet disease |
| Interferon beta 1a and 1b | Class II recombinant cytokines used to treat MS. |
| Interferon gamma b | Class III recombinant cytokines that promote CTL responses. Tx-Chronic granulomatous disease. |
| Aldesleukin | Recombinant IL-2 used to promote lymphocyte differentiation for cell-mediated response and activating natural killer cells. Tx-adjuvant renal cell carcinoma, metastatic melanoma. SE-capillary leak syndrome and cardiovascular toxicity. |
| Oprelvekin | recombinant IL-11 used to stimulate platelet formation. Tx-thrombocytopenia. |
| Filgrastim | recombinant G-CSF (neupogen) used to increase neutrophil production from peripheral blood stem cells and enhances phagocytic and cytotoxic effects of neutrophils.Tx- post-op BMT or chemotherapy recovery. |
| Sargramostim | recombinant GM-CSF (Prokine;Leukine) stimulates both granulocyte and macrophage progenitor cells to mature. Tx-myeloid recovery for high dose chemotherapy, AIDs associated neutropenia. CI-heart failure, pulmonary edema, and yeast hypersensitivity. |
| Epoetin-alfa | recombinant EPO that stimulates erythroid precursors and erythropoesis. Tx-anemia w/ adjuvant iron supplementation. SE-heart and liver toxicity associated with long term use. |
| Thrombopoetin | Recombinant myeloid cytokine growth factor analogous to G-CSF/EPO/GM-CSF. often fused w/ IL-3 and GM-CSF to stimulate megakaryocytopoiesis tx-high-dose chemotherapy. by itslf tx-accelerated platelet recovery after BMT |
| Immunosuppressives toxic to all dividing cells | Asithioprine |
| Immunosuppressives toxic to lymphocytes. | antilymphocytic globulin (ALG;ATG), immunoglobulin (IV), Rho (D) immunoglobulin, Muromonab-CD3, Asparaginase, Glucocorticoids. |
| Immunosuppressives toxic to a sub population of immune cells. | Cyclosporine, Tacrolimus, sirolimus, micophenylate mofetil. |
| Molecular target immunosuppressives. | Etranercept-receptor that binds cytokine. |
| Monoclonal antibodies which bind to cytokines w/ toxic outcome | Infliximab and daclizumab |
| Bisphosphonates used for osteoporosis Tx | Alendronate, risedronate, ibandronate, zoledronate, pamidronate. |
| RANKL antagonist used for osteoporosis Tx | Denosumab |
| Selective estrogen receptor modulator (SERM) used for osteoporosis Tx. | Raloxifene |
| Recombinant PTH used for osteoporosis Tx. | Teriparatide |
| Bisphosphonates | pyrophosphate --> hydroxyapatite --> osteocalst endocytosis --> inhibits prenylation of enzymes (GTPases)--> apoptosis. 1st line Tx and prevention of osteoporosis, glucocorticoid-induced osteoporosis, pagets disease, & hypercalcemia of malignancy. |
| Bisphosphonate adverse effects (SE) and contraindications (CI) | SE-erosive esophagitis, renal impairment, osteonecrosis of the jaw. CI-decreased renal function, esophageal motility disorder, peptic ulcer disease. |
| Denosumab | monoclonal antibody against RANKL which reduces osteoclast numbers and bone resorption. Tx-fracture prevention in post-menopausal women w/ osteoporosis who have impaired renal function or are unresponsive to other drugs. |
| Teriparatide | PTH analog w/ chronically high doses causing bone resorption, but moderate dose spikes causing bone formation. Given SC. Tx-severe osteogenesis T score<3.5 and w/ Hx of fractures, failure or intolerance to bisphosphonates. AE-osteosarcoma risk |
| Calcitonin | inhibtis osteoclastic activity by directly binding osteoclasts. Given intranasally or SC. Tx-osteoporosis, hypercalcemia of malignancy, pagets disease. SE-short acting, hypersensitivity. |
| Raloxifene | bind and activate estrogen receptor --> inhibiton of cytokines that activate osteoclasts, decrease osteoclast lifespan, increase osteoblast recruitment. Tx- osteoporosis w/ breast cancer or high risk. SE- thromboembolism, hot flashes. |
| Antiretroviral NRT1 drugs | Stavudine, abacavir, lamivudine, tenofovir, emtricitibine, didanosine, zidovudine |
| Antiretroviral NNRT1 drugs | Dalaviridine, efavirenz, nevirapine |
| Antiretroviral PI drugs | Saquinavir, atazanavir, indinavir, lopinavir, rotinavir |
| Antiretroviral entry inhibitor drugs | Efuviritide (GP41); maraviroc (CCR5) |
| Antiretroviral integrase inhibtor drugs | Raltegravir |
| HIV-1 and HIV-2 treatment that requires intracytoplasmic activation via phosphorylation to a triphosphate form to competitively inhibits HIV reverse transcriptase. Has mitochondrial toxicity and lactic acidosis adverse effects. | stavudine, abacavir, lamivudine, tenofavir, emtricitabine, didanosine, zidovudine |
| HIV-1 specific treatment with no phosphorylation steps and highly metabolized and eliminated by CYP450. Binds HIV-1 reverse transcriptase resulting in allosteric, noncompetitive inhibition of the enzyme. | Dalaviridine, efavirenz, nevirapine |
| No intracellular activation is required but is extensively metabolized by CYP3A4. Treatment of HIV-1 and HIV-2 by competitively inhibiting HIV aspartyl protease. Inhibits CYP3A4 and redistributes body fat, increases LDL/triglyceride, hyperglycemia. | Saquinavir, atazanavir, indinavir, lopinavir, Ritonavir |
| Given SC 2X/day to treat HIV-1 specifically by binding gp41 to prevent fusion and inhibit CD4 and cell-to-cell HIV transmission.Treats therapy-experienced adults and children >6y/o. causes injection site reaction. | Efuviritide |
| Taken orally to bind specifically to CCR5 to block CCR5-tropic R5 HIV-1 gp120 binding.URis, arthritis/musculoskeletal symptoms, and hepatotoxicity are potential SAs. | maraviroc |
| Oral pyrimidinone treating HIV-1 and HIV-2 by inhibiting integrase. Total cholesterol is increased and suicidality are potential side affects. | Raltegravir |
| Given to prevent the transmission of HIV to newborns from mothers or post-occupational exposure prophylaxis. | Zidovudine and Nevirapine |
| Peptidomimetic that is used as an inhibitor of CYP34A in combination with PIs to decrease frequency of dosing, increase tolerability, and increase potency. May have life-threatening drug interactions. | Ritonavir |
| Taken on an empty stomach due to gastric acid inactivating the drug and has highest risk to cause pancreatitis and optic neuritis | Didanosine |
| HIV medications that can also be used in the treatment of HBV. | lamivudine, tenofovir, emtricitabine |
| List the best combination of NNRTI + 2 NRTIs for treatment of HIV. | Efavirenz + tenofovir/emtricitabine |
| List the best combination of booster PI + 2 NRTIs for treatment of HIV. | Atazanavir/Ritonavir + tenofovir/emtricitabine |
| List the best combination of integrase inhibitor + 2 NRTI's | Raltegravir + tenofovir/emtricatabine |
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